Keerti Jain - Academia.edu (original) (raw)
Papers by Keerti Jain
Journal of Drug Delivery Science and Technology, 2021
Abstract Bedaquiline fumarate (BDQN) is approved in year 2012 to treat multidrug resistance tuber... more Abstract Bedaquiline fumarate (BDQN) is approved in year 2012 to treat multidrug resistance tuberculosis (MDR-TB) through accelerated approval pathway by FDA. It belongs to class II of biopharmaceutical classification system (BCS) and shows poor aqueous solubility and dissolution rate which eventually leads to compromised bioavailability. In the present study, BDQN loaded binary solid dispersion (BSD) and ternary solid dispersion (TSD) were prepared with the aid of solvent evaporation technique wherein poloxamer 188 and tocopheryl polyethylene glycol 1000 succinate (TPGS) were used as dispersing matrix. The prepared BSD and TSD were characterized by dynamic light scattering (DLS), attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), hot stage microscopy (HSM), powder X-ray diffraction (PXRD), and evaluated for enhancement in saturation solubility, in vitro dissolution performance, and permeability through rat intestine. BSD and TSD showed 5.68-fold and 7.46-fold increment in saturation solubility respectively. In vitro dissolution data showed about 99.98 ± 1.48% BDQN release from BSD within 15 min (t15 min, %) and, 98.68 ± 1.98% release from TSD within 30 min (t30 min, %) which were significantly higher than that of BDQN plain drug and their respective physical mixtures at respective time points. However, BSD was unable to sustain the parachute effect of BDQN in dissolution medium and showed decreased concentrations whereas TSD maintained the same throughout experimental period. Permeability of BDQN from BSD and TSD was found to be 1.86-fold and 3.53-fold, respectively, when compared to BDQN plain drug. TSD was found to be stable at accelerated condition for the period of 3 months when evaluated by PXRD, FTIR, DSC and in vitro dissolution study. We may conclude from this study that solid dispersions of BDQN can be accepted as promising alternative formulation approach to enhance biopharmaceutical performance of BDQN in terms of solubility, dissolution rate and permeability for treatment of tuberculosis and may benefit the patients with MDR-TB for the emergency treatment with BDQN, which could ultimately lead to increase in bioavailability and reduced cost of final product.
Biopolymer-Based Composites, 2017
Dendrimers have attracted growing attention in the field of drug delivery as smart nanoengineered... more Dendrimers have attracted growing attention in the field of drug delivery as smart nanoengineered polymers. They are defined as novel three-dimensional polymers with nearly monodispersed architectures with well-defined size and shape. Dendrimers are synthesized by step-by-step controlled chemical reactions. Because of their unique properties, exclusive synthesis methods, distinctive architecture, monodispersity, and physicochemical properties, dendrimers are emerging as smart, tailor-made, safe, and effective nanoengineered polymers for biomedical applications. In the current scenario dendrimers are extensively being investigated as bioinspired polymers for various drug delivery applications to achieve controlled delivery as well as to develop personalized medicine systems. They have shown potential as intracellular delivery vector to achieve therapeutic concentration at cellular targets with enhanced specificity. Furthermore, dendrimers have also shown their applicability in tissue engineering. Dendrimers have been explored in the controlled and targeted delivery of a large number of bioactives, including anticancer drugs, antiviral drugs, antileishmanial drugs, small interfering RNA, gene, antigens, and diagnostic and contrast agents. Unmodified dendrimers with surface cationic groups may elicit some toxic manifestations, and the surface engineering of dendrimers to mask these cationic surface groups plays a critical role in their possible clinical applications by rendering them a more biocompatible surface with less toxicity. Dendrimers are being explored for a vast array of biomedical applications, and in this chapter we have given an account on the various aspects of this nanoengineered polymer, particularly in relevance to its drug delivery applications.
Molecules, 2021
Clean and safe water is a fundamental human need for multi-faceted development of society and a t... more Clean and safe water is a fundamental human need for multi-faceted development of society and a thriving economy. Brisk rises in populations, expanding industrialization, urbanization and extensive agriculture practices have resulted in the generation of wastewater which have not only made the water dirty or polluted, but also deadly. Millions of people die every year due to diseases communicated through consumption of water contaminated by deleterious pathogens. Although various methods for wastewater treatment have been explored in the last few decades but their use is restrained by many limitations including use of chemicals, formation of disinfection by-products (DBPs), time consumption and expensiveness. Nanotechnology, manipulation of matter at a molecular or an atomic level to craft new structures, devices and systems having superior electronic, optical, magnetic, conductive and mechanical properties, is emerging as a promising technology, which has demonstrated remarkable fe...
Journal of Nanoparticle Research, 2021
Treating diseases of the central nervous system (CNS) still remains a problem for the researchers... more Treating diseases of the central nervous system (CNS) still remains a problem for the researchers. Existence of specific anatomical barriers, especially the blood brain barrier (BBB), restricts the brain mobility and hinders the effectiveness of different drug therapies. Rapid nanotechnological developments have given promising solutions to this challenge. Therefore, during the last few decades, a variety of nanocarriers have been designed to deliver drugs to the brain. Dendrimers are highly branched, three-dimensional macromolecules with tailor-made surface functionality and internal cavities that make them interesting carrier to deliver the drug to the brain. Significant advances have been made in dendrimer-mediated targeted delivery to the brain in last two decades. This review article deals majorly with recent advances in dendrimer-mediated delivery to the brain with discussions on the mechanisms of biodistribution and toxicity of dendrimer crossing the BBB. This will assist researchers in designing the new strategies to deal with major challenges related to the targeted delivery of CNS therapeutic agents to the brain.
Drug Discovery Today, 2019
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
Pharmaceutical Nanotechnology, 2019
Most of the active pharmaceutical ingredient used in the management of disease have poor water so... more Most of the active pharmaceutical ingredient used in the management of disease have poor water solubility and offer grueling problems in drug formulation development since low solubility is generally associated with poor dissolution characteristics which leads to poor oral bioavailability. The great challenge for the development of a pharmaceutical product is to create its new formulation and drug delivery system to limit solubility problems of existing drug candidate. Limited drug-loading capacity requires a large amount of carrier material to get appropriate encapsulation of the drug, which is another major challenge in the development of pharmaceutical product which could be resolved by developing nanocrystals (NCs). A significant research in the past few years has been done to develop NCs which helps in the delivery of poorly water soluble drugs via different routes. The technology could continue to thrive as a useful tool in pharmaceutical sciences for the improvement of drug s...
Current Pharmaceutical Design, 2019
Background: Personalized medicines are becoming more popular as they enable the use of patient’s ... more Background: Personalized medicines are becoming more popular as they enable the use of patient’s genomics and hence help in better drug design with fewer side effects. In fact, several doses can be combined into one dosage form which suits the patient’s demography. 3 Dimensional (3D) printing technology for personalized medicine is a modern day treatment method based on genomics of patient. Methods: 3D printing technology uses digitally controlled devices for formulating API and excipients in a layer by layer pattern for developing a suitable personalized drug delivery system as per the need of patient. It includes various techniques like inkjet printing, fused deposition modelling which can further be classified into continuous inkjet system and drop on demand. In order to formulate such dosage forms, scientists have used various polymers to enhance their acceptance as well as therapeutic efficacy. Polymers like polyvinyl alcohol, poly (lactic acid) (PLA), poly (caprolactone) (PCL)...
Recent Patents on Anti-Infective Drug Discovery, 2018
Background: Acne vulgaris is a common chronic skin disease that affects around 9.4% (approx. 650 ... more Background: Acne vulgaris is a common chronic skin disease that affects around 9.4% (approx. 650 million people) of the global population. Growing research in the field of nanomedicine over the years has now been exploited in management of various human disorders. The nanomedicine concept has an immense opportunity for the effective management and control of acne disease by designing a novel, low-dose topical delivery system. Topical nanoemulsion-based gel preparations are said to have various benefits over the conventional formulations. The recent patents on topical anti-acne formulation (US 7241456B2; US 6897238B2; US 6284234B1) provided the concept to design thymol loaded nano-emulgel for topical application in acne. Methods: The objective of the current investigation was to design a thymol loaded nanoemulgel preparation by exploiting low-energy emulsification method for topical application in acne. Furthermore, developed formulation was characterized for thermodynamic stability,...
Journal of Tourism & Hospitality, 2017
Journal of Colloid Science and Biotechnology, 2015
Artificial Cells, Nanomedicine, and Biotechnology, 2016
In this study, we reported folate-conjugated polypropylene imine dendrimers (FA-PPI) as efficient... more In this study, we reported folate-conjugated polypropylene imine dendrimers (FA-PPI) as efficient carrier for model anticancer drug, methotrexate (MTX), for pH-sensitive drug release, selective targeting to cancer cells, and anticancer activity. In the in vitro drug release studies this nanoconjugate of MTX showed initial rapid release followed by gradual slow release, and the drug release was found to be pH sensitive with greater release at acidic pH. The ex vivo investigations with human breast cancer cell lines, MCF-7, showed enhanced cytotoxicity of MTX-FA-PPI with significantly enhanced intracellular uptake. The biofate of nanoconjugate was determined in Wistar rat where MTX-FA-PPI showed 37.79-fold increase in the concentration of MTX in liver after 24 h in comparison with free MTX formulation.
Encyclopedia of Biomedical Polymers and Polymeric Biomaterials, 2016
Artificial Cells, Nanomedicine, and Biotechnology, 2016
The main aim of the present investigation was to explore the effect of functionalization on drug ... more The main aim of the present investigation was to explore the effect of functionalization on drug delivery potential of carbon nanotubes (CNTs) and to compare the in vitro and in vivo cancer targeting potential of doxorubicin HCL (DOX)-loaded ox-/multi-walled CNTs (MWCNTs), DOX-loaded PEG-MWCNTs and DOX-loaded FA-PEG-MWCNTs. The DOX/PEG-FA-MWCNTs showed enhanced cytotoxicity and were most preferentially taken up by the cancerous cells. The obtained results also support the extended resistance time and sustained release profile of drug-loaded surface-engineered MWCNTs. Overall, we concluded that the developed MWCNTs nanoformulations have higher cancer targeting potential.
Current Pharmaceutical Design, 2015
Journal of Nanoparticle Research, 2015
The aim of the present investigation was to deliver Gemcitabine Hydrochloride (GmcH), an anticanc... more The aim of the present investigation was to deliver Gemcitabine Hydrochloride (GmcH), an anticancer bioactive, specifically to lung tumor cells using mannosylated 4.0G poly(propyleneimine) dendrimers (M-PPI). 4.0G poly(propyleneimine) (PPI) dendrimers was synthesized using ethylenediamine as core and conjugated with mannose by ring opening reactions, followed by Schiff’s reaction in the presence of sodium acetate buffer (pH 4.0). Synthesized PPI dendrimers and mannose-conjugated dendrimers were characterized using IR, NMR spectroscopy, and scanning electron microscopy. GmcH was loaded into PPI and M-PPI dendrimers using equilibrium dialysis method to develop the formulations, GmcH-PPI and GmcH-M-PPI, respectively. The developed formulations were evaluated for drug loading, in vitro release kinetics, in vitro stability, hemolytic toxicity, cytotoxicity, pharmacokinetic, and biodistribution studies. The dendrimeric formulation of GmcH showed pH-sensitive release with faster release at acidic pH, i.e., pH 4.0 in comparison with physiological pH 7.4. M-PPI conjugate showed significant reduction in hemolytic toxicity as compared to plain 4.0G PPI dendrimers towards human erythrocytes. In the cytotoxicity studies with A-549 lung adenocarcinoma cell line, the GmcH-M-PPI formulation showed the lowest IC50 value. Further, the pharmacokinetic and tissue distribution studies of free drug GmcH, GmcH-PPI, and GmcH-M-PPI in albino rats of Sprague–Dawley strain suggested the mean residence time of GmcH-M-PPI conjugate to be significantly higher (24.85 h) than free GmcH and GmcH-PPI. Deposition of drug (396.1 ± 4.7 after 2 h) in lung was found to be significantly higher with GmcH-M-PPI formulation in comparison with Gmch and GmcH-PPI.
Artificial Cells, Nanomedicine, and Biotechnology, 2015
We herein first report a method for the synthesis of chitosan (CHI)-folate conjugated colloidal Z... more We herein first report a method for the synthesis of chitosan (CHI)-folate conjugated colloidal ZnO-Mn(+2) quantum dots (QDs) bearing doxorubicin through chemical method (DOX/FA-CHI-QDs) for cancer therapy as well imaging purpose. The entrapment efficiency was determined to be 99.98 ± 0.012% (DOX/FA-CHI-QDs) and 92.0 ± 2.62% (DOX-QDs). The developed DOX/FA-CHI-QDs formulations depict the sustained release pattern at the lysosomal pH (pH 5.0). The DOX/FA-CHI-QDs showed enhanced cytotoxicity, cellular uptake and were most preferentially taken up by the cancerous cells via receptor-mediated endocytosis (RME) mechanism. Hence, the QD-based formulation is capable of targeting drug delivery and imaging the delivery process.
Journal of immunological methods, Jan 6, 2015
Visceral leishmaniasis, which is also known as Kala-Azar, is one the most severe neglected tropic... more Visceral leishmaniasis, which is also known as Kala-Azar, is one the most severe neglected tropical diseases recognized by World Health Organization (WHO). The threat of this debilitating disease is continued due to unavailability of promising drug therapy or human vaccine. An extensive research is undergoing to develop a promising vaccine to prevent this devastating disease. In this review we compiled the findings of recent research with a view to facilitate knowledge on experimental vaccinology for visceral leishmaniasis. Various killed or attenuated parasite based first generation vaccines, second generation vaccines based on antigenic protein or recombinant protein, and third generation vaccines derived from antigen-encoding DNA plasmids including heterologous prime-boost Leishmania vaccine have been examined for control and prevention of visceral leishmaniasis. Vaccines based on recombinant protein and antigen-encoding DNA plasmids have given promising results and few vaccines ...
Journal of Drug Delivery Science and Technology, 2021
Abstract Bedaquiline fumarate (BDQN) is approved in year 2012 to treat multidrug resistance tuber... more Abstract Bedaquiline fumarate (BDQN) is approved in year 2012 to treat multidrug resistance tuberculosis (MDR-TB) through accelerated approval pathway by FDA. It belongs to class II of biopharmaceutical classification system (BCS) and shows poor aqueous solubility and dissolution rate which eventually leads to compromised bioavailability. In the present study, BDQN loaded binary solid dispersion (BSD) and ternary solid dispersion (TSD) were prepared with the aid of solvent evaporation technique wherein poloxamer 188 and tocopheryl polyethylene glycol 1000 succinate (TPGS) were used as dispersing matrix. The prepared BSD and TSD were characterized by dynamic light scattering (DLS), attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), hot stage microscopy (HSM), powder X-ray diffraction (PXRD), and evaluated for enhancement in saturation solubility, in vitro dissolution performance, and permeability through rat intestine. BSD and TSD showed 5.68-fold and 7.46-fold increment in saturation solubility respectively. In vitro dissolution data showed about 99.98 ± 1.48% BDQN release from BSD within 15 min (t15 min, %) and, 98.68 ± 1.98% release from TSD within 30 min (t30 min, %) which were significantly higher than that of BDQN plain drug and their respective physical mixtures at respective time points. However, BSD was unable to sustain the parachute effect of BDQN in dissolution medium and showed decreased concentrations whereas TSD maintained the same throughout experimental period. Permeability of BDQN from BSD and TSD was found to be 1.86-fold and 3.53-fold, respectively, when compared to BDQN plain drug. TSD was found to be stable at accelerated condition for the period of 3 months when evaluated by PXRD, FTIR, DSC and in vitro dissolution study. We may conclude from this study that solid dispersions of BDQN can be accepted as promising alternative formulation approach to enhance biopharmaceutical performance of BDQN in terms of solubility, dissolution rate and permeability for treatment of tuberculosis and may benefit the patients with MDR-TB for the emergency treatment with BDQN, which could ultimately lead to increase in bioavailability and reduced cost of final product.
Biopolymer-Based Composites, 2017
Dendrimers have attracted growing attention in the field of drug delivery as smart nanoengineered... more Dendrimers have attracted growing attention in the field of drug delivery as smart nanoengineered polymers. They are defined as novel three-dimensional polymers with nearly monodispersed architectures with well-defined size and shape. Dendrimers are synthesized by step-by-step controlled chemical reactions. Because of their unique properties, exclusive synthesis methods, distinctive architecture, monodispersity, and physicochemical properties, dendrimers are emerging as smart, tailor-made, safe, and effective nanoengineered polymers for biomedical applications. In the current scenario dendrimers are extensively being investigated as bioinspired polymers for various drug delivery applications to achieve controlled delivery as well as to develop personalized medicine systems. They have shown potential as intracellular delivery vector to achieve therapeutic concentration at cellular targets with enhanced specificity. Furthermore, dendrimers have also shown their applicability in tissue engineering. Dendrimers have been explored in the controlled and targeted delivery of a large number of bioactives, including anticancer drugs, antiviral drugs, antileishmanial drugs, small interfering RNA, gene, antigens, and diagnostic and contrast agents. Unmodified dendrimers with surface cationic groups may elicit some toxic manifestations, and the surface engineering of dendrimers to mask these cationic surface groups plays a critical role in their possible clinical applications by rendering them a more biocompatible surface with less toxicity. Dendrimers are being explored for a vast array of biomedical applications, and in this chapter we have given an account on the various aspects of this nanoengineered polymer, particularly in relevance to its drug delivery applications.
Molecules, 2021
Clean and safe water is a fundamental human need for multi-faceted development of society and a t... more Clean and safe water is a fundamental human need for multi-faceted development of society and a thriving economy. Brisk rises in populations, expanding industrialization, urbanization and extensive agriculture practices have resulted in the generation of wastewater which have not only made the water dirty or polluted, but also deadly. Millions of people die every year due to diseases communicated through consumption of water contaminated by deleterious pathogens. Although various methods for wastewater treatment have been explored in the last few decades but their use is restrained by many limitations including use of chemicals, formation of disinfection by-products (DBPs), time consumption and expensiveness. Nanotechnology, manipulation of matter at a molecular or an atomic level to craft new structures, devices and systems having superior electronic, optical, magnetic, conductive and mechanical properties, is emerging as a promising technology, which has demonstrated remarkable fe...
Journal of Nanoparticle Research, 2021
Treating diseases of the central nervous system (CNS) still remains a problem for the researchers... more Treating diseases of the central nervous system (CNS) still remains a problem for the researchers. Existence of specific anatomical barriers, especially the blood brain barrier (BBB), restricts the brain mobility and hinders the effectiveness of different drug therapies. Rapid nanotechnological developments have given promising solutions to this challenge. Therefore, during the last few decades, a variety of nanocarriers have been designed to deliver drugs to the brain. Dendrimers are highly branched, three-dimensional macromolecules with tailor-made surface functionality and internal cavities that make them interesting carrier to deliver the drug to the brain. Significant advances have been made in dendrimer-mediated targeted delivery to the brain in last two decades. This review article deals majorly with recent advances in dendrimer-mediated delivery to the brain with discussions on the mechanisms of biodistribution and toxicity of dendrimer crossing the BBB. This will assist researchers in designing the new strategies to deal with major challenges related to the targeted delivery of CNS therapeutic agents to the brain.
Drug Discovery Today, 2019
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
Pharmaceutical Nanotechnology, 2019
Most of the active pharmaceutical ingredient used in the management of disease have poor water so... more Most of the active pharmaceutical ingredient used in the management of disease have poor water solubility and offer grueling problems in drug formulation development since low solubility is generally associated with poor dissolution characteristics which leads to poor oral bioavailability. The great challenge for the development of a pharmaceutical product is to create its new formulation and drug delivery system to limit solubility problems of existing drug candidate. Limited drug-loading capacity requires a large amount of carrier material to get appropriate encapsulation of the drug, which is another major challenge in the development of pharmaceutical product which could be resolved by developing nanocrystals (NCs). A significant research in the past few years has been done to develop NCs which helps in the delivery of poorly water soluble drugs via different routes. The technology could continue to thrive as a useful tool in pharmaceutical sciences for the improvement of drug s...
Current Pharmaceutical Design, 2019
Background: Personalized medicines are becoming more popular as they enable the use of patient’s ... more Background: Personalized medicines are becoming more popular as they enable the use of patient’s genomics and hence help in better drug design with fewer side effects. In fact, several doses can be combined into one dosage form which suits the patient’s demography. 3 Dimensional (3D) printing technology for personalized medicine is a modern day treatment method based on genomics of patient. Methods: 3D printing technology uses digitally controlled devices for formulating API and excipients in a layer by layer pattern for developing a suitable personalized drug delivery system as per the need of patient. It includes various techniques like inkjet printing, fused deposition modelling which can further be classified into continuous inkjet system and drop on demand. In order to formulate such dosage forms, scientists have used various polymers to enhance their acceptance as well as therapeutic efficacy. Polymers like polyvinyl alcohol, poly (lactic acid) (PLA), poly (caprolactone) (PCL)...
Recent Patents on Anti-Infective Drug Discovery, 2018
Background: Acne vulgaris is a common chronic skin disease that affects around 9.4% (approx. 650 ... more Background: Acne vulgaris is a common chronic skin disease that affects around 9.4% (approx. 650 million people) of the global population. Growing research in the field of nanomedicine over the years has now been exploited in management of various human disorders. The nanomedicine concept has an immense opportunity for the effective management and control of acne disease by designing a novel, low-dose topical delivery system. Topical nanoemulsion-based gel preparations are said to have various benefits over the conventional formulations. The recent patents on topical anti-acne formulation (US 7241456B2; US 6897238B2; US 6284234B1) provided the concept to design thymol loaded nano-emulgel for topical application in acne. Methods: The objective of the current investigation was to design a thymol loaded nanoemulgel preparation by exploiting low-energy emulsification method for topical application in acne. Furthermore, developed formulation was characterized for thermodynamic stability,...
Journal of Tourism & Hospitality, 2017
Journal of Colloid Science and Biotechnology, 2015
Artificial Cells, Nanomedicine, and Biotechnology, 2016
In this study, we reported folate-conjugated polypropylene imine dendrimers (FA-PPI) as efficient... more In this study, we reported folate-conjugated polypropylene imine dendrimers (FA-PPI) as efficient carrier for model anticancer drug, methotrexate (MTX), for pH-sensitive drug release, selective targeting to cancer cells, and anticancer activity. In the in vitro drug release studies this nanoconjugate of MTX showed initial rapid release followed by gradual slow release, and the drug release was found to be pH sensitive with greater release at acidic pH. The ex vivo investigations with human breast cancer cell lines, MCF-7, showed enhanced cytotoxicity of MTX-FA-PPI with significantly enhanced intracellular uptake. The biofate of nanoconjugate was determined in Wistar rat where MTX-FA-PPI showed 37.79-fold increase in the concentration of MTX in liver after 24 h in comparison with free MTX formulation.
Encyclopedia of Biomedical Polymers and Polymeric Biomaterials, 2016
Artificial Cells, Nanomedicine, and Biotechnology, 2016
The main aim of the present investigation was to explore the effect of functionalization on drug ... more The main aim of the present investigation was to explore the effect of functionalization on drug delivery potential of carbon nanotubes (CNTs) and to compare the in vitro and in vivo cancer targeting potential of doxorubicin HCL (DOX)-loaded ox-/multi-walled CNTs (MWCNTs), DOX-loaded PEG-MWCNTs and DOX-loaded FA-PEG-MWCNTs. The DOX/PEG-FA-MWCNTs showed enhanced cytotoxicity and were most preferentially taken up by the cancerous cells. The obtained results also support the extended resistance time and sustained release profile of drug-loaded surface-engineered MWCNTs. Overall, we concluded that the developed MWCNTs nanoformulations have higher cancer targeting potential.
Current Pharmaceutical Design, 2015
Journal of Nanoparticle Research, 2015
The aim of the present investigation was to deliver Gemcitabine Hydrochloride (GmcH), an anticanc... more The aim of the present investigation was to deliver Gemcitabine Hydrochloride (GmcH), an anticancer bioactive, specifically to lung tumor cells using mannosylated 4.0G poly(propyleneimine) dendrimers (M-PPI). 4.0G poly(propyleneimine) (PPI) dendrimers was synthesized using ethylenediamine as core and conjugated with mannose by ring opening reactions, followed by Schiff’s reaction in the presence of sodium acetate buffer (pH 4.0). Synthesized PPI dendrimers and mannose-conjugated dendrimers were characterized using IR, NMR spectroscopy, and scanning electron microscopy. GmcH was loaded into PPI and M-PPI dendrimers using equilibrium dialysis method to develop the formulations, GmcH-PPI and GmcH-M-PPI, respectively. The developed formulations were evaluated for drug loading, in vitro release kinetics, in vitro stability, hemolytic toxicity, cytotoxicity, pharmacokinetic, and biodistribution studies. The dendrimeric formulation of GmcH showed pH-sensitive release with faster release at acidic pH, i.e., pH 4.0 in comparison with physiological pH 7.4. M-PPI conjugate showed significant reduction in hemolytic toxicity as compared to plain 4.0G PPI dendrimers towards human erythrocytes. In the cytotoxicity studies with A-549 lung adenocarcinoma cell line, the GmcH-M-PPI formulation showed the lowest IC50 value. Further, the pharmacokinetic and tissue distribution studies of free drug GmcH, GmcH-PPI, and GmcH-M-PPI in albino rats of Sprague–Dawley strain suggested the mean residence time of GmcH-M-PPI conjugate to be significantly higher (24.85 h) than free GmcH and GmcH-PPI. Deposition of drug (396.1 ± 4.7 after 2 h) in lung was found to be significantly higher with GmcH-M-PPI formulation in comparison with Gmch and GmcH-PPI.
Artificial Cells, Nanomedicine, and Biotechnology, 2015
We herein first report a method for the synthesis of chitosan (CHI)-folate conjugated colloidal Z... more We herein first report a method for the synthesis of chitosan (CHI)-folate conjugated colloidal ZnO-Mn(+2) quantum dots (QDs) bearing doxorubicin through chemical method (DOX/FA-CHI-QDs) for cancer therapy as well imaging purpose. The entrapment efficiency was determined to be 99.98 ± 0.012% (DOX/FA-CHI-QDs) and 92.0 ± 2.62% (DOX-QDs). The developed DOX/FA-CHI-QDs formulations depict the sustained release pattern at the lysosomal pH (pH 5.0). The DOX/FA-CHI-QDs showed enhanced cytotoxicity, cellular uptake and were most preferentially taken up by the cancerous cells via receptor-mediated endocytosis (RME) mechanism. Hence, the QD-based formulation is capable of targeting drug delivery and imaging the delivery process.
Journal of immunological methods, Jan 6, 2015
Visceral leishmaniasis, which is also known as Kala-Azar, is one the most severe neglected tropic... more Visceral leishmaniasis, which is also known as Kala-Azar, is one the most severe neglected tropical diseases recognized by World Health Organization (WHO). The threat of this debilitating disease is continued due to unavailability of promising drug therapy or human vaccine. An extensive research is undergoing to develop a promising vaccine to prevent this devastating disease. In this review we compiled the findings of recent research with a view to facilitate knowledge on experimental vaccinology for visceral leishmaniasis. Various killed or attenuated parasite based first generation vaccines, second generation vaccines based on antigenic protein or recombinant protein, and third generation vaccines derived from antigen-encoding DNA plasmids including heterologous prime-boost Leishmania vaccine have been examined for control and prevention of visceral leishmaniasis. Vaccines based on recombinant protein and antigen-encoding DNA plasmids have given promising results and few vaccines ...