Arkendu Chatterjee - Academia.edu (original) (raw)
Papers by Arkendu Chatterjee
Journal of Ophthalmic and Vision Research, 2019
Purpose: To evaluate the efficacy, safety, and steroid-sparing effect of topical cyclosporine A (... more Purpose: To evaluate the efficacy, safety, and steroid-sparing effect of topical cyclosporine A (Cs A) 0.05% in patients with moderate to severe steroid dependent vernal keratoconjunctivitis (VKC). Methods: A prospective, comparative, placebo controlled study was carried out on 68 VKC patients, with 34 patients treated with topical Cs A 0.05% and the remaining 34 with topical carboxymethyl cellulose 0.5% (placebo). Both groups also received topical loteprednol etabonate 0.5%. Symptom (itching, photophobia, tearing, and discharge) score, sign (tarsal and limbal papillae, corneal involvement, and conjunctival hyperemia) score, and drug score (steroid drop usage/day/eye) were recorded at baseline and each followup visit. The intraocular pressure (IOP) measurement and evaluation of any ocular side effects were carried out. Results: Significant reduction in symptom score and sign score was seen in both groups. Cs A group significantly showed more reduction in symptom (P < 0.0001 in al...
Journal of the Indian Medical Association, 2011
Choroidal haemangioma is a benign tumour with visual acuity diminution due to subretinal fluid ac... more Choroidal haemangioma is a benign tumour with visual acuity diminution due to subretinal fluid accumulation. There are many modalities of treatment of this visually disabling syndrome, some of them being argon laser photocoagulation, cryotherapy, external beam irradiation, proton beam radiotherapy, episcleral plaque radiotherapy and transpupillary thermotherapy. Another new modality of treatment with remarkable success rate is photodynamic therapy. In this modality a photosensitiser is injected intravenously followed by irradiation of a specific wave length for a specified time period. The photosensitiser concentrates within the vascular channels and after irradiation these channels are irreversibly obliterated. A 62 years old female patient of choroidal haemangioma, who presented in eye outpatient department was treated with the standard protocol used for photodynamic therapy. On follow-up of this patient it was found that there was improvement in the visual acuity from 6/12 in the...
Journal of the Indian Medical Association, 2012
To study the macular thickness and peripapillary nerve fibre layer thickness in children with ani... more To study the macular thickness and peripapillary nerve fibre layer thickness in children with anisometropic amblyopia, a prospective non-randomised case series study was undertaken among 39 children (25 boys and 14 girls) aged between 5 and 16 years. This study was carried out between January 2010 and April 2011. The peripapillary retinal nerve fibre layer (RNFL) thickness and macular layer thickness was measured using optical coherence tomography (OCT), the RNFL thickness and the macular layer thickness of the amblyopic eye was assessed and compared to the normal eye of the same subject. It was found that macular layer thickness in the amblyopic eye was greater than that of the macular thickness in the normal eye. The mean macular layer thickness in the amblyopic eyes was 229.589 microm with a standard deviation of -+/- 31.9149 microm. The mean macular layer thickness in the normal eyes of these children was 206.8717 microm with a standard deviation of +/- 28.490 microm, the p-valu...
Journal of the Indian Medical Association, 2011
A prospective, non-randomised, interventional case series study was designed among 127 specimens ... more A prospective, non-randomised, interventional case series study was designed among 127 specimens obtained from 100 consecutive patients presenting with primary pterygium attending the outpatient department of a teaching hospital in Kolkata, West Bengal between September 2009 and August 2010. After harvesting the pterygium it was transported in 10% formol saline for staining, fixing and embedding prior to evaluation of tissue alkaline phosphatase level and estimation of DNA content in nucleus of cells in pterygium tissue. The main outcome was to measure alkaline phosphatase activity and DNA content in pterygium tissue and normal bulbar conjunctiva along with histopathological staining and to see if any correlation exists between alkaline phosphatase activity and DNA content of pterygium tissue in different stages of evolution as suggested by histological staining. The elastic proliferation and hyaline degeneration are prominent in well developed pterygium. The alkaline phosphatase ac...
Saudi Journal of Ophthalmology, 2015
Frontal osteomyelitis is a rare clinical entity that can occur as sequelae to frontal sinusitis, ... more Frontal osteomyelitis is a rare clinical entity that can occur as sequelae to frontal sinusitis, head trauma, as a postoperative complication following sinus surgery or due to haematogenous spread. It usually presents with a soft, fluctuant forehead swelling with pain and fever. Cicatricial ectropion is an extremely rare feature of frontal osteomyelitis. We present a young male patient presenting with cicatricial ectropion that occurred as the sole manifestation of an underlying frontal osteomyelitis. Extensive Medline search did not find any such reported case. We feel that frontal osteomyelitis should be kept in mind as a possible etiology when considering the differential diagnosis of cicatricial ectropion.
Exhaustive efforts have been made to the administration of drugs, via alternative routes, that ar... more Exhaustive efforts have been made to the administration of drugs, via alternative routes, that are poorly absorbed after the oral administration. The vaginal route of drug delivery has been known since ancient times. In recent years, the vaginal route has been rediscovered as a potential route for systemic delivery of peptides and other therapeutically important macromolecules. However, successful delivery of drugs through the vagina remains a challenge, primarily due to the poor absorption across the vaginal epithelium. The rate and extent of drug absorption after intra vaginal administration may vary depending on formulation factors, vaginal physiology, age of the patient and menstrual cycle. Suppositories, creams, gels, tablets and vaginal rings are commonly used vaginal drug delivery systems. The purpose of this communication is to provide the reader with a summary of advances made in the field of vaginal drug delivery. This report, therefore, summarizes various vaginal drug del...
Abstract: The main aim of present research is to increase the bioavailability of Lisinopril by fo... more Abstract: The main aim of present research is to increase the bioavailability of Lisinopril by formulating it as Transdermal patches to avoid its first pass metabolism. Total six formulations were prepared by using two different polymers like PVA and HPMC K15M in three different concentrations. F3 formulation with 8% of PVA was selected as best optimized formulation
Some drugs are poorly absorbed after the oral administration. Over the last twenty years, extensi... more Some drugs are poorly absorbed after the oral administration. Over the last twenty years, extensive efforts have been made towards the administration of poorly absorbed drugs through different delivery systems and routes but the presence of a mucus laden cervix (vagina) in women provides an opportunity as a conjoint site for such drug delivery. The vaginal route has been rediscovered as a potential route for systemic delivery of various therapeutically important drugs avoid first pass metabolism. However, fruitful delivery of drugs through the vagina remains a challenge because of poor absorption of some drugs across vaginal epithelium. The various factors like vaginal physiology, age of patient, menstrual cycle are affecting the rate of drug absorption after vaginal administration. The future of vaginal drug delivery lies in the bioadhesive tablets, liposomes, niosomes and microparticles, which although relatively new and show great promise in providing truly controlled delivery of...
... 147 SUSTAINED RELEASE DRUG DELIVERY SYSTEM : A REVIEW Shalin A. Modi1*, PD Gaikwad1, VH Banka... more ... 147 SUSTAINED RELEASE DRUG DELIVERY SYSTEM : A REVIEW Shalin A. Modi1*, PD Gaikwad1, VH Bankar1, SP Pawar1 1P.SGVPM's College of Pharmacy, Shahada, Dist-Nandurbar, Maharashtra-425 409 Email:sam_pharmacist@rediffmail.com ABSTRACT ...
American Journal of PharmTech Research
The main goal is to identify suitable to their Anti-hypertensive activity with reference (Clonidi... more The main goal is to identify suitable to their Anti-hypertensive activity with reference (Clonidine Standard drug). Pubchem webserver, Chemsketch, Padel descriptor, Protein data bank (PDB), Autodocktools, E-dragon webserver. To generate the Scaffold molecule. To calculate different parameters of test sample with its biological activity. To fit the final series of compound with particular target. To predict ADMET of final series of compound. After substitution R 1 & R 2 of test sample we have found that the value of different descriptors of QSARs is nearby equal to standard drug of clonidine. All the descriptors are (QSARs parameters) of Scaffold molecule H 1 was satisfactorily explained (R 2 = Approximately 0.99) with the graphical plot of Hansch analysis. This compound had very poor blood brain barrier crossing label, good absorption, no hepatotoxicity, no mutagenecity. Beside this compound was non-carconogenic after in-silico predictions of ADMET.
International Journal of Advanced Research in Biological Sciences (IJARBS)
Computer-aided drug design (CADD) depends on the extent of structure and other information availa... more Computer-aided drug design (CADD) depends on the extent of structure and other information available regarding the target (enzyme/receptor/protein) and the ligands. The theoretical basis of CADD involves molecular mechanics, quantum mechanics, molecular dynamics, structure-based drug design (SBDD), ligand-based drug design (LBDD), homology modeling, ligplot analysis, molecular docking, de novo drug design, pharmacophore modeling and mapping, virtual screening (VS), quantitative structure-activity relationships (QSARs), In silico ADMET (absorption, distribution, metabolism, excretion and toxicity) prediction etc. CADD centre was created to foster collaborative research between biologist, biophysicists, structural biologists and computational scientists. The major goal of the CADD centre is to initiate these collaborations leading to the establishment of research projects to discover novel chemical entities with the potential to be developed into novel therapeutic agents.
Pharmaceutical Development and Technology
The aim of this study was to develop and evaluate a Zidovudine (AZT)-loaded microparticulated bio... more The aim of this study was to develop and evaluate a Zidovudine (AZT)-loaded microparticulated bioadhesive vaginal gel (MBVG) in order to obtain a controlled releasing, safe gel delivery system. AZT microparticles (ZMPs) were evaluated for encapsulation efficiency, drug loading, surface morphology and in vitro drug release profiles and drug release mechanism and optimized. The optimized ZMPs were then encompassed in bioadhesive gel using different bioadhesive polymers and evaluated for the drug encapsulation efficiency, drug loading, in vitro and in vivo drug release profiles, drug release mechanism and vaginal irritancy study. From the dissolution data of ZMP4 and MBVG4 showed a zero-order diffusion pattern and Fickian diffusion case I transport mechanism in 24 and 36 h, respectively. On the basis of a pharmacokinetic study of MBVG4 (containing ZMP: Carbopol 1:4), it was found to have better bioavailability, larger AUC and Tmax in comparison to an oral pure suspension of AZT.
Hydrogel is a network of polymer chains that are water-insoluble, sometimes found as a colloidal ... more Hydrogel is a network of polymer chains that are water-insoluble, sometimes found as a colloidal gel in which water is the dispersion medium. Hydrogels are crosslinked polymer networks that absorb substantial amounts of aqueous solutions. Due to their high water content, these gels resemble natural living tissue more than any other type of synthetic biomaterial. Several techniques have been reported for the synthesis of hydrogels like co polymerization/crosslinking of co-monomers using multifunctional co-monomer, which acts as crosslinking agent. Chemical initiator initiates the polymerization reaction. Some applications are used of hydrogels in human body. Some environmental variables, such as low pH and elevated temperatures, are found in the body. For this reason, either pH-sensitive and/or temperature sensitive hydrogels can be used for site-specific controlled drug delivery. Hydrogels that are responsive to specific molecules, such as glucose or antigens, can be used as biosens...
Gel as a dosage forms are successfully used as drug delivery systems which considering their abil... more Gel as a dosage forms are successfully used as drug delivery systems which considering their ability to prolong the drug release. HIV microbicides are topical, self-administered products aimed to preventing or reducing HIV infection in women and may represent the most promising strategy for combating the HIV/AIDS epidemic at the present time. Drug delivery across vagina, is a challenging task. Keeping this view, a new vaginal anti-HIV microencapsulated vaginal gel (AZMBVG) was engineered to coat vaginal tissue with a stable HIV protective layer. Ideally, drug will be release from this gel layer to improve controlled fashion due to presence of microcapsules and bioadhesive polymers. The whole work was divided between two phases. In first phase, Zidovudine loaded microcapsules (AZMC) were prepared by O/O single emulsion solvent evaporation method. The encapsulation efficiency was observed into the range of 15.37 ± 0.45 to 93.92 ± 4.59 %.The FTIR study showed that no chemical interacti...
Bioadhesion in vagina is a topic of current interest in the design of particulated bioadhesive ge... more Bioadhesion in vagina is a topic of current interest in the design of particulated bioadhesive gel as drug delivery systems and different evaluations. Particulate carrier systems comprising of nanoparticles, liposomes, niosomes, microparticulates etc. are incorporated with bioadhesive gel, exhibit a prolong residence time at the site of application or absorption and hence facilitate an intimate contact with the vaginal epithelial membrane to improve the therapeutic performance of the drug. In recent years such vaginal gels are used in different diseases. The principles underlying the formulation development and characterization of particulated bioadhesive gel and the current research trends in this arena are explored in this review.
The objective of the present study was to formulation development, characterize and in vitro drug... more The objective of the present study was to formulation development, characterize and in vitro drug release efficacy of microencapsulated bio adhesive vaginal tablet (MBVT) for treatment of AIDS. The microcapsules were prepared by the solvent evaporation method, were characterized for the percent drug content, entrapment efficiency, micromeritic analysis, FTIR, surface morphology and in vitro dissolution studies. The microcapsules were compressed into in tablet by direct compression method, after blending with the bioadhesive polymers and other formulation additives. The MBVTs were evaluated for average weight, hardness, friability, drug content, bioadhesion test, swelling index study of tablet formulation and in-vitro drug release study. The microcapsules were found to be discrete with entrapment efficiency of 67.12-99.1%. FTIR study showed the no chemical interaction between drug and polymer. SEM revealed that the microcapsules were porous in nature. In vitro drug release study of m...
Gel as a dosage forms are successfully used as drug delivery systems which considering their abil... more Gel as a dosage forms are successfully used as drug delivery systems which considering their ability to prolong the drug release. HIV microbicides are topical, self-administered products aimed to preventing or reducing HIV infection in women and may represent the most promising strategy for combating the HIV/AIDS epidemic at the present time. Drug delivery across vagina, is a challenging task. Keeping this view, a new vaginal anti-HIV microencapsulated vaginal gel (AZMBVG) was engineered to coat vaginal tissue with a stable HIV protective layer. Ideally, drug will be release from this gel layer to improve controlled fashion due to presence of microcapsules and bioadhesive polymers. The whole work was divided between two phases. In first phase, Zidovudine loaded microcapsules (AZMC) were prepared by O/O single emulsion solvent evaporation method. The encapsulation efficiency was observed into the range of 15.37 ± 0.45 to 93.92 ± 4.59 %. The FTIR study showed that no chemical interact...
A study was conducted on the antifungal (Tinea pedis) activity of Heliotropium indicum Linn. It w... more A study was conducted on the antifungal (Tinea pedis) activity of Heliotropium indicum Linn. It was found that methanolic hexane and aqueous extract have shown some antifungal activity. We are also fractionating the aqueous extract to acidic, basic and neutral portion. The neutral fraction is also active compared to standard whereas acidic and basic fractions are not active. Aqueous extract is found to be more active compared to methanol, hexane and neutral fraction. Aqueous extract of Heliotropium indicum showed antifungal activity with lowest inhibitory concentration (MIC) of 8 mg/ml. The neutral portion of aqueous extract was also found with some antifungal activity shown by zone of inhibition. It was observed that the acidic and basic portions of the aqueous extracts were not active on Tinea pedis and MIC of the neutral portion was found to be 18.6 mg/ml.
Journal of Young Pharmacists, 2011
Inexpensive and female-controlled pre-exposure prophylaxis strategies to prevent mucosal transmis... more Inexpensive and female-controlled pre-exposure prophylaxis strategies to prevent mucosal transmission of the virus, is urgently needed with the rising prevalence of human immunodeficiency virus (HIV-1 and HIV2) infections in women. Zidovudine-loaded bioadhesive vaginal gel may become one of the very useful strategies, as it can be used not only for controlled release but also for enhancing bioavailability. Drug delivery through vaginal gel is a promising area for continued research with the aim of achieving controlled release with enhanced bioavailability over longer periods of time. The aim of the study was to develop a newer prolong releasing Zidovudine (AZT) bioadhesive vaginal gel to treat HIV infections with increased patient convenience. AZT-loaded bioadhesive vaginal gel was prepared successfully by using cold mechanical method. F3 formulation containing carbopol-HPMC (1:3) was selected and evaluated in order to achieve objectives of this study. In vitro drug release study of F3 showed in 24 h drug released following case I Fickian (n ≤ 0.5) transport mechanism, and in vivo drug release was found much better (T max), (C max), and bioavailability (F) comparison with oral pour drug solution. It was also showed good extrudability, spreadability, and bioadhesive strength. A generalized protocol, for the further research, in this area will surely expected to yield significant outcome with improved drug delivery system.
ijpsr.com
The present study concerned with the development and characterization of bioadhesive vaginal film... more The present study concerned with the development and characterization of bioadhesive vaginal film (VF). Zidovudine containing VF were prepared by solvent casting method using different ratios of Acrycoat S 100 (AC) or Ethyl cellulose (EC) to Hydroxy propyl methyl cellulose (HPMC) and di butyl phthalate(DBP) as a plasticizer. The optimized films were found to be transparent, flexible and soft and evaluated for mechanical properties by modified instrument, drug content, folding endurance, in vitro drug release with release kinetic and % moisture content bioadhesive strength by modified pan balance method. The films were found higher drug content and flexible. The VF10 (containing AC: HPMC 4:1) was selected. In vitro drug was found of Zidovudine over 11 hr obeying zero order followed by Higuchi kinetics and Case II non-Fickian (anomalous) diffusion control, indicating the rate of drug release is due to the combined effect of drug diffusion and polymer relaxation with a sufficient bio adhesion quality with good mechanical properties. The results were compared statistically and found with satisfactory correlation. Thus in conclusion preparation protocol of VFs studied may be adopted for a successful development of newer drug delivery system for treatment and prevention for AIDS.
Journal of Ophthalmic and Vision Research, 2019
Purpose: To evaluate the efficacy, safety, and steroid-sparing effect of topical cyclosporine A (... more Purpose: To evaluate the efficacy, safety, and steroid-sparing effect of topical cyclosporine A (Cs A) 0.05% in patients with moderate to severe steroid dependent vernal keratoconjunctivitis (VKC). Methods: A prospective, comparative, placebo controlled study was carried out on 68 VKC patients, with 34 patients treated with topical Cs A 0.05% and the remaining 34 with topical carboxymethyl cellulose 0.5% (placebo). Both groups also received topical loteprednol etabonate 0.5%. Symptom (itching, photophobia, tearing, and discharge) score, sign (tarsal and limbal papillae, corneal involvement, and conjunctival hyperemia) score, and drug score (steroid drop usage/day/eye) were recorded at baseline and each followup visit. The intraocular pressure (IOP) measurement and evaluation of any ocular side effects were carried out. Results: Significant reduction in symptom score and sign score was seen in both groups. Cs A group significantly showed more reduction in symptom (P < 0.0001 in al...
Journal of the Indian Medical Association, 2011
Choroidal haemangioma is a benign tumour with visual acuity diminution due to subretinal fluid ac... more Choroidal haemangioma is a benign tumour with visual acuity diminution due to subretinal fluid accumulation. There are many modalities of treatment of this visually disabling syndrome, some of them being argon laser photocoagulation, cryotherapy, external beam irradiation, proton beam radiotherapy, episcleral plaque radiotherapy and transpupillary thermotherapy. Another new modality of treatment with remarkable success rate is photodynamic therapy. In this modality a photosensitiser is injected intravenously followed by irradiation of a specific wave length for a specified time period. The photosensitiser concentrates within the vascular channels and after irradiation these channels are irreversibly obliterated. A 62 years old female patient of choroidal haemangioma, who presented in eye outpatient department was treated with the standard protocol used for photodynamic therapy. On follow-up of this patient it was found that there was improvement in the visual acuity from 6/12 in the...
Journal of the Indian Medical Association, 2012
To study the macular thickness and peripapillary nerve fibre layer thickness in children with ani... more To study the macular thickness and peripapillary nerve fibre layer thickness in children with anisometropic amblyopia, a prospective non-randomised case series study was undertaken among 39 children (25 boys and 14 girls) aged between 5 and 16 years. This study was carried out between January 2010 and April 2011. The peripapillary retinal nerve fibre layer (RNFL) thickness and macular layer thickness was measured using optical coherence tomography (OCT), the RNFL thickness and the macular layer thickness of the amblyopic eye was assessed and compared to the normal eye of the same subject. It was found that macular layer thickness in the amblyopic eye was greater than that of the macular thickness in the normal eye. The mean macular layer thickness in the amblyopic eyes was 229.589 microm with a standard deviation of -+/- 31.9149 microm. The mean macular layer thickness in the normal eyes of these children was 206.8717 microm with a standard deviation of +/- 28.490 microm, the p-valu...
Journal of the Indian Medical Association, 2011
A prospective, non-randomised, interventional case series study was designed among 127 specimens ... more A prospective, non-randomised, interventional case series study was designed among 127 specimens obtained from 100 consecutive patients presenting with primary pterygium attending the outpatient department of a teaching hospital in Kolkata, West Bengal between September 2009 and August 2010. After harvesting the pterygium it was transported in 10% formol saline for staining, fixing and embedding prior to evaluation of tissue alkaline phosphatase level and estimation of DNA content in nucleus of cells in pterygium tissue. The main outcome was to measure alkaline phosphatase activity and DNA content in pterygium tissue and normal bulbar conjunctiva along with histopathological staining and to see if any correlation exists between alkaline phosphatase activity and DNA content of pterygium tissue in different stages of evolution as suggested by histological staining. The elastic proliferation and hyaline degeneration are prominent in well developed pterygium. The alkaline phosphatase ac...
Saudi Journal of Ophthalmology, 2015
Frontal osteomyelitis is a rare clinical entity that can occur as sequelae to frontal sinusitis, ... more Frontal osteomyelitis is a rare clinical entity that can occur as sequelae to frontal sinusitis, head trauma, as a postoperative complication following sinus surgery or due to haematogenous spread. It usually presents with a soft, fluctuant forehead swelling with pain and fever. Cicatricial ectropion is an extremely rare feature of frontal osteomyelitis. We present a young male patient presenting with cicatricial ectropion that occurred as the sole manifestation of an underlying frontal osteomyelitis. Extensive Medline search did not find any such reported case. We feel that frontal osteomyelitis should be kept in mind as a possible etiology when considering the differential diagnosis of cicatricial ectropion.
Exhaustive efforts have been made to the administration of drugs, via alternative routes, that ar... more Exhaustive efforts have been made to the administration of drugs, via alternative routes, that are poorly absorbed after the oral administration. The vaginal route of drug delivery has been known since ancient times. In recent years, the vaginal route has been rediscovered as a potential route for systemic delivery of peptides and other therapeutically important macromolecules. However, successful delivery of drugs through the vagina remains a challenge, primarily due to the poor absorption across the vaginal epithelium. The rate and extent of drug absorption after intra vaginal administration may vary depending on formulation factors, vaginal physiology, age of the patient and menstrual cycle. Suppositories, creams, gels, tablets and vaginal rings are commonly used vaginal drug delivery systems. The purpose of this communication is to provide the reader with a summary of advances made in the field of vaginal drug delivery. This report, therefore, summarizes various vaginal drug del...
Abstract: The main aim of present research is to increase the bioavailability of Lisinopril by fo... more Abstract: The main aim of present research is to increase the bioavailability of Lisinopril by formulating it as Transdermal patches to avoid its first pass metabolism. Total six formulations were prepared by using two different polymers like PVA and HPMC K15M in three different concentrations. F3 formulation with 8% of PVA was selected as best optimized formulation
Some drugs are poorly absorbed after the oral administration. Over the last twenty years, extensi... more Some drugs are poorly absorbed after the oral administration. Over the last twenty years, extensive efforts have been made towards the administration of poorly absorbed drugs through different delivery systems and routes but the presence of a mucus laden cervix (vagina) in women provides an opportunity as a conjoint site for such drug delivery. The vaginal route has been rediscovered as a potential route for systemic delivery of various therapeutically important drugs avoid first pass metabolism. However, fruitful delivery of drugs through the vagina remains a challenge because of poor absorption of some drugs across vaginal epithelium. The various factors like vaginal physiology, age of patient, menstrual cycle are affecting the rate of drug absorption after vaginal administration. The future of vaginal drug delivery lies in the bioadhesive tablets, liposomes, niosomes and microparticles, which although relatively new and show great promise in providing truly controlled delivery of...
... 147 SUSTAINED RELEASE DRUG DELIVERY SYSTEM : A REVIEW Shalin A. Modi1*, PD Gaikwad1, VH Banka... more ... 147 SUSTAINED RELEASE DRUG DELIVERY SYSTEM : A REVIEW Shalin A. Modi1*, PD Gaikwad1, VH Bankar1, SP Pawar1 1P.SGVPM's College of Pharmacy, Shahada, Dist-Nandurbar, Maharashtra-425 409 Email:sam_pharmacist@rediffmail.com ABSTRACT ...
American Journal of PharmTech Research
The main goal is to identify suitable to their Anti-hypertensive activity with reference (Clonidi... more The main goal is to identify suitable to their Anti-hypertensive activity with reference (Clonidine Standard drug). Pubchem webserver, Chemsketch, Padel descriptor, Protein data bank (PDB), Autodocktools, E-dragon webserver. To generate the Scaffold molecule. To calculate different parameters of test sample with its biological activity. To fit the final series of compound with particular target. To predict ADMET of final series of compound. After substitution R 1 & R 2 of test sample we have found that the value of different descriptors of QSARs is nearby equal to standard drug of clonidine. All the descriptors are (QSARs parameters) of Scaffold molecule H 1 was satisfactorily explained (R 2 = Approximately 0.99) with the graphical plot of Hansch analysis. This compound had very poor blood brain barrier crossing label, good absorption, no hepatotoxicity, no mutagenecity. Beside this compound was non-carconogenic after in-silico predictions of ADMET.
International Journal of Advanced Research in Biological Sciences (IJARBS)
Computer-aided drug design (CADD) depends on the extent of structure and other information availa... more Computer-aided drug design (CADD) depends on the extent of structure and other information available regarding the target (enzyme/receptor/protein) and the ligands. The theoretical basis of CADD involves molecular mechanics, quantum mechanics, molecular dynamics, structure-based drug design (SBDD), ligand-based drug design (LBDD), homology modeling, ligplot analysis, molecular docking, de novo drug design, pharmacophore modeling and mapping, virtual screening (VS), quantitative structure-activity relationships (QSARs), In silico ADMET (absorption, distribution, metabolism, excretion and toxicity) prediction etc. CADD centre was created to foster collaborative research between biologist, biophysicists, structural biologists and computational scientists. The major goal of the CADD centre is to initiate these collaborations leading to the establishment of research projects to discover novel chemical entities with the potential to be developed into novel therapeutic agents.
Pharmaceutical Development and Technology
The aim of this study was to develop and evaluate a Zidovudine (AZT)-loaded microparticulated bio... more The aim of this study was to develop and evaluate a Zidovudine (AZT)-loaded microparticulated bioadhesive vaginal gel (MBVG) in order to obtain a controlled releasing, safe gel delivery system. AZT microparticles (ZMPs) were evaluated for encapsulation efficiency, drug loading, surface morphology and in vitro drug release profiles and drug release mechanism and optimized. The optimized ZMPs were then encompassed in bioadhesive gel using different bioadhesive polymers and evaluated for the drug encapsulation efficiency, drug loading, in vitro and in vivo drug release profiles, drug release mechanism and vaginal irritancy study. From the dissolution data of ZMP4 and MBVG4 showed a zero-order diffusion pattern and Fickian diffusion case I transport mechanism in 24 and 36 h, respectively. On the basis of a pharmacokinetic study of MBVG4 (containing ZMP: Carbopol 1:4), it was found to have better bioavailability, larger AUC and Tmax in comparison to an oral pure suspension of AZT.
Hydrogel is a network of polymer chains that are water-insoluble, sometimes found as a colloidal ... more Hydrogel is a network of polymer chains that are water-insoluble, sometimes found as a colloidal gel in which water is the dispersion medium. Hydrogels are crosslinked polymer networks that absorb substantial amounts of aqueous solutions. Due to their high water content, these gels resemble natural living tissue more than any other type of synthetic biomaterial. Several techniques have been reported for the synthesis of hydrogels like co polymerization/crosslinking of co-monomers using multifunctional co-monomer, which acts as crosslinking agent. Chemical initiator initiates the polymerization reaction. Some applications are used of hydrogels in human body. Some environmental variables, such as low pH and elevated temperatures, are found in the body. For this reason, either pH-sensitive and/or temperature sensitive hydrogels can be used for site-specific controlled drug delivery. Hydrogels that are responsive to specific molecules, such as glucose or antigens, can be used as biosens...
Gel as a dosage forms are successfully used as drug delivery systems which considering their abil... more Gel as a dosage forms are successfully used as drug delivery systems which considering their ability to prolong the drug release. HIV microbicides are topical, self-administered products aimed to preventing or reducing HIV infection in women and may represent the most promising strategy for combating the HIV/AIDS epidemic at the present time. Drug delivery across vagina, is a challenging task. Keeping this view, a new vaginal anti-HIV microencapsulated vaginal gel (AZMBVG) was engineered to coat vaginal tissue with a stable HIV protective layer. Ideally, drug will be release from this gel layer to improve controlled fashion due to presence of microcapsules and bioadhesive polymers. The whole work was divided between two phases. In first phase, Zidovudine loaded microcapsules (AZMC) were prepared by O/O single emulsion solvent evaporation method. The encapsulation efficiency was observed into the range of 15.37 ± 0.45 to 93.92 ± 4.59 %.The FTIR study showed that no chemical interacti...
Bioadhesion in vagina is a topic of current interest in the design of particulated bioadhesive ge... more Bioadhesion in vagina is a topic of current interest in the design of particulated bioadhesive gel as drug delivery systems and different evaluations. Particulate carrier systems comprising of nanoparticles, liposomes, niosomes, microparticulates etc. are incorporated with bioadhesive gel, exhibit a prolong residence time at the site of application or absorption and hence facilitate an intimate contact with the vaginal epithelial membrane to improve the therapeutic performance of the drug. In recent years such vaginal gels are used in different diseases. The principles underlying the formulation development and characterization of particulated bioadhesive gel and the current research trends in this arena are explored in this review.
The objective of the present study was to formulation development, characterize and in vitro drug... more The objective of the present study was to formulation development, characterize and in vitro drug release efficacy of microencapsulated bio adhesive vaginal tablet (MBVT) for treatment of AIDS. The microcapsules were prepared by the solvent evaporation method, were characterized for the percent drug content, entrapment efficiency, micromeritic analysis, FTIR, surface morphology and in vitro dissolution studies. The microcapsules were compressed into in tablet by direct compression method, after blending with the bioadhesive polymers and other formulation additives. The MBVTs were evaluated for average weight, hardness, friability, drug content, bioadhesion test, swelling index study of tablet formulation and in-vitro drug release study. The microcapsules were found to be discrete with entrapment efficiency of 67.12-99.1%. FTIR study showed the no chemical interaction between drug and polymer. SEM revealed that the microcapsules were porous in nature. In vitro drug release study of m...
Gel as a dosage forms are successfully used as drug delivery systems which considering their abil... more Gel as a dosage forms are successfully used as drug delivery systems which considering their ability to prolong the drug release. HIV microbicides are topical, self-administered products aimed to preventing or reducing HIV infection in women and may represent the most promising strategy for combating the HIV/AIDS epidemic at the present time. Drug delivery across vagina, is a challenging task. Keeping this view, a new vaginal anti-HIV microencapsulated vaginal gel (AZMBVG) was engineered to coat vaginal tissue with a stable HIV protective layer. Ideally, drug will be release from this gel layer to improve controlled fashion due to presence of microcapsules and bioadhesive polymers. The whole work was divided between two phases. In first phase, Zidovudine loaded microcapsules (AZMC) were prepared by O/O single emulsion solvent evaporation method. The encapsulation efficiency was observed into the range of 15.37 ± 0.45 to 93.92 ± 4.59 %. The FTIR study showed that no chemical interact...
A study was conducted on the antifungal (Tinea pedis) activity of Heliotropium indicum Linn. It w... more A study was conducted on the antifungal (Tinea pedis) activity of Heliotropium indicum Linn. It was found that methanolic hexane and aqueous extract have shown some antifungal activity. We are also fractionating the aqueous extract to acidic, basic and neutral portion. The neutral fraction is also active compared to standard whereas acidic and basic fractions are not active. Aqueous extract is found to be more active compared to methanol, hexane and neutral fraction. Aqueous extract of Heliotropium indicum showed antifungal activity with lowest inhibitory concentration (MIC) of 8 mg/ml. The neutral portion of aqueous extract was also found with some antifungal activity shown by zone of inhibition. It was observed that the acidic and basic portions of the aqueous extracts were not active on Tinea pedis and MIC of the neutral portion was found to be 18.6 mg/ml.
Journal of Young Pharmacists, 2011
Inexpensive and female-controlled pre-exposure prophylaxis strategies to prevent mucosal transmis... more Inexpensive and female-controlled pre-exposure prophylaxis strategies to prevent mucosal transmission of the virus, is urgently needed with the rising prevalence of human immunodeficiency virus (HIV-1 and HIV2) infections in women. Zidovudine-loaded bioadhesive vaginal gel may become one of the very useful strategies, as it can be used not only for controlled release but also for enhancing bioavailability. Drug delivery through vaginal gel is a promising area for continued research with the aim of achieving controlled release with enhanced bioavailability over longer periods of time. The aim of the study was to develop a newer prolong releasing Zidovudine (AZT) bioadhesive vaginal gel to treat HIV infections with increased patient convenience. AZT-loaded bioadhesive vaginal gel was prepared successfully by using cold mechanical method. F3 formulation containing carbopol-HPMC (1:3) was selected and evaluated in order to achieve objectives of this study. In vitro drug release study of F3 showed in 24 h drug released following case I Fickian (n ≤ 0.5) transport mechanism, and in vivo drug release was found much better (T max), (C max), and bioavailability (F) comparison with oral pour drug solution. It was also showed good extrudability, spreadability, and bioadhesive strength. A generalized protocol, for the further research, in this area will surely expected to yield significant outcome with improved drug delivery system.
ijpsr.com
The present study concerned with the development and characterization of bioadhesive vaginal film... more The present study concerned with the development and characterization of bioadhesive vaginal film (VF). Zidovudine containing VF were prepared by solvent casting method using different ratios of Acrycoat S 100 (AC) or Ethyl cellulose (EC) to Hydroxy propyl methyl cellulose (HPMC) and di butyl phthalate(DBP) as a plasticizer. The optimized films were found to be transparent, flexible and soft and evaluated for mechanical properties by modified instrument, drug content, folding endurance, in vitro drug release with release kinetic and % moisture content bioadhesive strength by modified pan balance method. The films were found higher drug content and flexible. The VF10 (containing AC: HPMC 4:1) was selected. In vitro drug was found of Zidovudine over 11 hr obeying zero order followed by Higuchi kinetics and Case II non-Fickian (anomalous) diffusion control, indicating the rate of drug release is due to the combined effect of drug diffusion and polymer relaxation with a sufficient bio adhesion quality with good mechanical properties. The results were compared statistically and found with satisfactory correlation. Thus in conclusion preparation protocol of VFs studied may be adopted for a successful development of newer drug delivery system for treatment and prevention for AIDS.