Kailas Moravkar - Academia.edu (original) (raw)

Papers by Kailas Moravkar

Research paper thumbnail of Development and in vitro, ex vivo, in vivo investigation of curcumin loaded nanoparticles in management of dry eye disease

Journal of Drug Delivery Science and Technology

Research paper thumbnail of Nanomaterials Toxicology: An Overview

Research paper thumbnail of A concise summary of powder processing methodologies for flow enhancement

Research paper thumbnail of Extraction of rutin from tagetes erecta (Marigold) and preparation of peroral nano-suspension for effective antitussive/expectorant therapy

Carbohydrate Polymer Technologies and Applications

Research paper thumbnail of Fabrication of pioglitazone nanoparticles loaded polymeric dispersion for treatment of dry eye disease with in vitro and in vivo investigation

Journal of Drug Delivery Science and Technology

Research paper thumbnail of Novel approach for the formulation of excipient-less fixed dose combination (FDC) tablets by Hot Melt Extrusion (HME) technology using quality by design approach

Clinical Pharmacology & Biopharmaceutics, Jan 30, 2017

T he objectives of the present study were to investigate the properties of HME based tablets cont... more T he objectives of the present study were to investigate the properties of HME based tablets containing plain ibuprofenparacetamol FDC, without a single excipient and to compare it with marketed formulation by applying QbD approach. Paracetamol and ibuprofen were taken at drug/drug mass ratios (5:2). The prepared physical mixtures were extruded using a corotating twin-screw hot melt extrusion. Among the three tested independent variables in DOE, temperature and feeding rate most significantly affected the tensile strength and drug release from the tablet. The melt extruded granules were passed through a 250μm sieve. The maximum optimized ratio (85:5.5:100) determined by DOE was chosen for further analysis. DSC, XRD, SEM were carried out to determine physicochemical changes after melt granulation. The granules were characterized for particle size analysis, flow properties, granule strength. Tablets containing 500 mg paracetamol and 200 mg ibuprofen were compressed at 10.0kN compaction force. The tablets were characterized for tablet hardness, friability, disintegration time and dissolution study. All results were found to be within acceptable USP limits. The optimized extruded batch was stable at 400C, 75%RH for a period of 6 months without changing any dissolution rate and remained into amorphous state.

Research paper thumbnail of Traditional and Advanced Flow Characterization Techniques: A Platform Review for Development of Solid Dosage Form

Indian Journal of Pharmaceutical Sciences, 2020

Moravkar et al.: PReview on flow characterization techniques Preformulation studies like storage,... more Moravkar et al.: PReview on flow characterization techniques Preformulation studies like storage, transfer, fluidisation, and compaction, are subject to the excellent flowability of the powder. It is often required for proper operational management and consistent design of industrial processes. Two basics methods have been utilised to characterise the flow behaviour of bulk solids. Traditionally, powder has been evaluated in terms of simple and straight forward techniques like Hausner's ratio, Carr's index, bulk density, and angle of repose. Despite that, the results obtained in the traditional method lack predictability, reproducibility, sensitivity, and the actual association between the resulting data and flow behaviour. Henceforth the results varied for weight variation, content uniformity, and dissolution, etc. during the preparation of final dosage forms. To overcome these limitations of the traditional methods, the advanced techniques are being utilised to explore micro properties like the angle of internal friction, bulk density, flow function, yield loci, powder rheometry under precisely controlled conditions of consolidation stress. Ultimately these techniques help to design, choose suitable excipients, reduce time along with cost, and improve the health of society. This review focuses on some of the most commonly applied methods used in traditional and advanced shear cell testing techniques to measure the flow of powders.

Research paper thumbnail of “Comparative Study of Three Granulation Techniques: Moisture Assisted Granulation Technique, Roller Compaction and Hot Melt Extrusion Technique with Maltodextrin DE16, PVP K 12 and HPC as Polymeric Binders”

Indo American Journal of Pharmaceutical Research, 2016

Research paper thumbnail of Role of neurogenesis in regenerative medicine

Research paper thumbnail of Assessment of pharmaceutical powders flowability and comparative evaluation of lubricants on development of gastro retentive tablets: An application of powder flow tester

Journal of Drug Delivery Science and Technology, 2022

Research paper thumbnail of Crosslinked Porous Starch Particles--a Promising Carrier

Polimery w medycynie, 2015

UNLABELLED Background. Starch is one of the most potential natural polymers used for various bio ... more UNLABELLED Background. Starch is one of the most potential natural polymers used for various bio applications. Literature reports a num- ber of modification strategies such as physical, chemical, enzymatic and genetic to enhance the positive attributes and iron out the undesired features of neat starch. OBJECTIVES To synthesize a crosslinked porous starch (CPS) as an efficient cargo for the delivery of calcium carbonate in an efficiently controlled manner for the treatment of hyperphosphatemia. MATERIAL AND METHODS The CPS carrier was synthesized using a natural crosslinker, malic acid. The drug delivery system was formulated, followed by the in situ loading of calcium carbonate during the preparation of the CPS. The developed system was characterized with respect to FTIR, DSC, SEM, moisture content, zeta potential, encapsulation efficiency, phosphate binding efficiency and dissolution studies. RESULTS The developed formulation was observed to deliver calcium carbonate in an enteric...

Research paper thumbnail of Modified Fenugreek Gum for Solubility and Dissolution Rate Enhancement of Simvastatin

Simvastatin is a hypolipidemic BCS class II drug and has poor bioavailability due to low aqueous ... more Simvastatin is a hypolipidemic BCS class II drug and has poor bioavailability due to low aqueous solubility. Solid dispersion is the one of the most promising method for improving the water solubility and therefore the drug bioavailability. In this study, solid dispersion of Simvastatin was prepared using lab synthesized hydrophilic surface active polymer octenyl succinate fenugreek gum as a carrier by cosolvent precipitation method. Different batches of solid dispersion were prepared in varying drug polymer ratio. Prepared solid dispersions were evaluated for solubility and dissolution rate. It was found that solid dispersion prepared from drug polymer 1:0.1 weight ratio showed threefold increase in dissolution rate and solubility was also improved several fold in dissolving medium. Solid dispersion was characterized for physicochemical property by differential scanning calorimetry, scanning electron microscopy, FTIR and particle size distribution. The compilations of these results...

Research paper thumbnail of Development of sustained release Aceclofenac lipid matrix tablet using continuous melt granulation technique

American Journal of PharmTech Research, 2018

Research paper thumbnail of Effect of melt extrudability and melt binding efficiency of polyvinyl caprolactam polyvinyl acetate polyethylene glycol graft copolymer (Soluplus®) on release pattern of hydrophilic and high dose drugs

Materials Science and Engineering: C, 2019

Research paper thumbnail of Study the influence of formulation process parameters on solubility and dissolution enhancement of efavirenz solid solutions prepared by hot-melt extrusion: a QbD methodology

Drug Delivery and Translational Research, 2018

Research paper thumbnail of Application of moisture activated dry granulation (MADG) process to develop high dose immediate release (IR) formulations

Advanced Powder Technology, 2017

Abstract Moisture activated dry granulation (MADG) method was used to develop IR tablets with coh... more Abstract Moisture activated dry granulation (MADG) method was used to develop IR tablets with cohesive, fluffy and high dose drugs. To evaluate this approach, three drugs: metformin hydrochloride, acetaminophen and ferrous ascorbate were selected as model compound along with three binders: maltodextrin DE16, PVP K 12 and HPC. The granules were generated using MADG method and tablets were prepared using rotary tablet press. The granules and tablets were characterized for particle size analysis, flow properties, tablet hardness, friability, moisture content, dissolution study, disintegration time and stability study. All results were found to be within acceptable limits. Development of all formulation tablets were found as best fitted for an immediate release of Metformin hydrochloride, acetaminophen and ferrous ascorbate. MADG delivered a robust manufacturing process for generation of granules with excellent flowability. The tablets prepared using this method were found to show better content uniformity, good compactability and low friability. Use of this approach aids to lower the amount of excipients used to overcome physiochemical limitation of the drug substances and there side effects. Both drying and milling steps in wet granulation were not required for MADG process. MADG became a cost effective process which could lead to reduced total tablet size and also save time.

Research paper thumbnail of Biodegradable Porous Starch Spheres as a Novel Carrier for Enhancement of Dissolution Rate and Oral Bioavailability of Itraconazole

Current Drug Delivery, 2017

A biodegradable porous starch (BPS) was developed in order to improve dissolution and oral bioava... more A biodegradable porous starch (BPS) was developed in order to improve dissolution and oral bioavailability of Itraconazole as a poorly water-soluble antifungal drug. BPS was developed by converting native starch from hydrogel to alcogel by solvent exchange method. The developed BPS carrier was characterized by SEM and nitrogen adsorption/desorption analysis to understand surface morphology and porosity distribution respectively. Itraconazole (ITR) was loaded on BPS by adsorption mediated solvent evaporation method, which provides a hydrophilic matrix powder. This causes drug distribution within hydrophilic matrix of porous starch. Solid-state characterization of optimized batch (ITR/BPS-3) was performed using DSC, PXRD, FTIR, SEM and FTIR imaging. In vitro dissolution and in vivo pharmacokinetic studies were performed to evaluate therapeutic potential of ITR/BPS-3 system. In vitro studies of ITR: BPS-3 system revealed a burst effect in drug release (100%) compared to marketed product, which showed (93%) drug release at end of 60 min. Moreover, ITR/BPS-3 system showed improved oral bioavailability up to 3.93 fold and marketed product shows 3.12 fold compared to ITR. This effect is due to high surface area, improved wettability and reduced crystallinity of ITR due to its adsorption into BPS. A successful methodology was reported to prepare BPS from raw starch.

Research paper thumbnail of Crosslinked Porous Starch Particles--a Promising Carrier

Polimery w medycynie

Background. Starch is one of the most potential natural polymers used for various bio application... more Background. Starch is one of the most potential natural polymers used for various bio applications. Literature reports a num- ber of modification strategies such as physical, chemical, enzymatic and genetic to enhance the positive attributes and iron out the undesired features of neat starch. To synthesize a crosslinked porous starch (CPS) as an efficient cargo for the delivery of calcium carbonate in an efficiently controlled manner for the treatment of hyperphosphatemia. The CPS carrier was synthesized using a natural crosslinker, malic acid. The drug delivery system was formulated, followed by the in situ loading of calcium carbonate during the preparation of the CPS. The developed system was characterized with respect to FTIR, DSC, SEM, moisture content, zeta potential, encapsulation efficiency, phosphate binding efficiency and dissolution studies. The developed formulation was observed to deliver calcium carbonate in an enterically controlled manner. The binding of calcium to p...

Research paper thumbnail of Exploring the potential of porous silicas as a carrier system for dissolution rate enhancement of artemether

Asian Journal of Pharmaceutical Sciences, 2016

Research paper thumbnail of Solubility and dissolution enhancement of efavirenz hot melt extruded amorphous solid dispersions using combination of polymeric blends: A QbD approach

European Journal of Pharmaceutical Sciences, 2016

Efavirenz is a non-nucleoside reverse transcriptase inhibitor and categorized in to BCS class II ... more Efavirenz is a non-nucleoside reverse transcriptase inhibitor and categorized in to BCS class II drug. The aim of the present investigation was to apply quality by design approach to enhance the solubility, dissolution and stability of amorphous solid dispersions (ASDs) of efavirenz using a combination of Soluplus® and HPMCAS-HF polymers. In design of experiments, the user defined quadratic model was used to study the effect of variable concentrations of Soluplus® and HPMCAS-HF for the formation of ASDs of efavirenz. Similarly, a prototype ASD was made using Soluplus® as a carrier with efavirenz loading of 30%. The efavirenz ASDs granular extrudates were evaluated for saturation solubility as well as dissolution rate studies. X-ray powder diffraction, Differential scanning calorimetry, Fourier transform infrared, Atomic force microscopy and FTIR imaging to determine the solid state of efavirenz in the ASDs. DSC and XRD data confirmed that bulk crystalline efavirenz transformed to the amorphous form during the hot melt extrusion processing. Prototype ASD batch showed instability upon storage as per ICH guidelines over a period of 6months, observations inferred from DSC, XRD and in vitro dissolution studies. The maximum dissolution rate was observed when Soluplus® and HPMCAS-HF was in ratio of (60:20) as optimized by design of experiments study. Moreover, the optimized ASDs batch were stable at 40°C, 75% RH for a period of 6months without any dissolution rate changes, and remained into amorphous state.

Research paper thumbnail of Development and in vitro, ex vivo, in vivo investigation of curcumin loaded nanoparticles in management of dry eye disease

Journal of Drug Delivery Science and Technology

Research paper thumbnail of Nanomaterials Toxicology: An Overview

Research paper thumbnail of A concise summary of powder processing methodologies for flow enhancement

Research paper thumbnail of Extraction of rutin from tagetes erecta (Marigold) and preparation of peroral nano-suspension for effective antitussive/expectorant therapy

Carbohydrate Polymer Technologies and Applications

Research paper thumbnail of Fabrication of pioglitazone nanoparticles loaded polymeric dispersion for treatment of dry eye disease with in vitro and in vivo investigation

Journal of Drug Delivery Science and Technology

Research paper thumbnail of Novel approach for the formulation of excipient-less fixed dose combination (FDC) tablets by Hot Melt Extrusion (HME) technology using quality by design approach

Clinical Pharmacology & Biopharmaceutics, Jan 30, 2017

T he objectives of the present study were to investigate the properties of HME based tablets cont... more T he objectives of the present study were to investigate the properties of HME based tablets containing plain ibuprofenparacetamol FDC, without a single excipient and to compare it with marketed formulation by applying QbD approach. Paracetamol and ibuprofen were taken at drug/drug mass ratios (5:2). The prepared physical mixtures were extruded using a corotating twin-screw hot melt extrusion. Among the three tested independent variables in DOE, temperature and feeding rate most significantly affected the tensile strength and drug release from the tablet. The melt extruded granules were passed through a 250μm sieve. The maximum optimized ratio (85:5.5:100) determined by DOE was chosen for further analysis. DSC, XRD, SEM were carried out to determine physicochemical changes after melt granulation. The granules were characterized for particle size analysis, flow properties, granule strength. Tablets containing 500 mg paracetamol and 200 mg ibuprofen were compressed at 10.0kN compaction force. The tablets were characterized for tablet hardness, friability, disintegration time and dissolution study. All results were found to be within acceptable USP limits. The optimized extruded batch was stable at 400C, 75%RH for a period of 6 months without changing any dissolution rate and remained into amorphous state.

Research paper thumbnail of Traditional and Advanced Flow Characterization Techniques: A Platform Review for Development of Solid Dosage Form

Indian Journal of Pharmaceutical Sciences, 2020

Moravkar et al.: PReview on flow characterization techniques Preformulation studies like storage,... more Moravkar et al.: PReview on flow characterization techniques Preformulation studies like storage, transfer, fluidisation, and compaction, are subject to the excellent flowability of the powder. It is often required for proper operational management and consistent design of industrial processes. Two basics methods have been utilised to characterise the flow behaviour of bulk solids. Traditionally, powder has been evaluated in terms of simple and straight forward techniques like Hausner's ratio, Carr's index, bulk density, and angle of repose. Despite that, the results obtained in the traditional method lack predictability, reproducibility, sensitivity, and the actual association between the resulting data and flow behaviour. Henceforth the results varied for weight variation, content uniformity, and dissolution, etc. during the preparation of final dosage forms. To overcome these limitations of the traditional methods, the advanced techniques are being utilised to explore micro properties like the angle of internal friction, bulk density, flow function, yield loci, powder rheometry under precisely controlled conditions of consolidation stress. Ultimately these techniques help to design, choose suitable excipients, reduce time along with cost, and improve the health of society. This review focuses on some of the most commonly applied methods used in traditional and advanced shear cell testing techniques to measure the flow of powders.

Research paper thumbnail of “Comparative Study of Three Granulation Techniques: Moisture Assisted Granulation Technique, Roller Compaction and Hot Melt Extrusion Technique with Maltodextrin DE16, PVP K 12 and HPC as Polymeric Binders”

Indo American Journal of Pharmaceutical Research, 2016

Research paper thumbnail of Role of neurogenesis in regenerative medicine

Research paper thumbnail of Assessment of pharmaceutical powders flowability and comparative evaluation of lubricants on development of gastro retentive tablets: An application of powder flow tester

Journal of Drug Delivery Science and Technology, 2022

Research paper thumbnail of Crosslinked Porous Starch Particles--a Promising Carrier

Polimery w medycynie, 2015

UNLABELLED Background. Starch is one of the most potential natural polymers used for various bio ... more UNLABELLED Background. Starch is one of the most potential natural polymers used for various bio applications. Literature reports a num- ber of modification strategies such as physical, chemical, enzymatic and genetic to enhance the positive attributes and iron out the undesired features of neat starch. OBJECTIVES To synthesize a crosslinked porous starch (CPS) as an efficient cargo for the delivery of calcium carbonate in an efficiently controlled manner for the treatment of hyperphosphatemia. MATERIAL AND METHODS The CPS carrier was synthesized using a natural crosslinker, malic acid. The drug delivery system was formulated, followed by the in situ loading of calcium carbonate during the preparation of the CPS. The developed system was characterized with respect to FTIR, DSC, SEM, moisture content, zeta potential, encapsulation efficiency, phosphate binding efficiency and dissolution studies. RESULTS The developed formulation was observed to deliver calcium carbonate in an enteric...

Research paper thumbnail of Modified Fenugreek Gum for Solubility and Dissolution Rate Enhancement of Simvastatin

Simvastatin is a hypolipidemic BCS class II drug and has poor bioavailability due to low aqueous ... more Simvastatin is a hypolipidemic BCS class II drug and has poor bioavailability due to low aqueous solubility. Solid dispersion is the one of the most promising method for improving the water solubility and therefore the drug bioavailability. In this study, solid dispersion of Simvastatin was prepared using lab synthesized hydrophilic surface active polymer octenyl succinate fenugreek gum as a carrier by cosolvent precipitation method. Different batches of solid dispersion were prepared in varying drug polymer ratio. Prepared solid dispersions were evaluated for solubility and dissolution rate. It was found that solid dispersion prepared from drug polymer 1:0.1 weight ratio showed threefold increase in dissolution rate and solubility was also improved several fold in dissolving medium. Solid dispersion was characterized for physicochemical property by differential scanning calorimetry, scanning electron microscopy, FTIR and particle size distribution. The compilations of these results...

Research paper thumbnail of Development of sustained release Aceclofenac lipid matrix tablet using continuous melt granulation technique

American Journal of PharmTech Research, 2018

Research paper thumbnail of Effect of melt extrudability and melt binding efficiency of polyvinyl caprolactam polyvinyl acetate polyethylene glycol graft copolymer (Soluplus®) on release pattern of hydrophilic and high dose drugs

Materials Science and Engineering: C, 2019

Research paper thumbnail of Study the influence of formulation process parameters on solubility and dissolution enhancement of efavirenz solid solutions prepared by hot-melt extrusion: a QbD methodology

Drug Delivery and Translational Research, 2018

Research paper thumbnail of Application of moisture activated dry granulation (MADG) process to develop high dose immediate release (IR) formulations

Advanced Powder Technology, 2017

Abstract Moisture activated dry granulation (MADG) method was used to develop IR tablets with coh... more Abstract Moisture activated dry granulation (MADG) method was used to develop IR tablets with cohesive, fluffy and high dose drugs. To evaluate this approach, three drugs: metformin hydrochloride, acetaminophen and ferrous ascorbate were selected as model compound along with three binders: maltodextrin DE16, PVP K 12 and HPC. The granules were generated using MADG method and tablets were prepared using rotary tablet press. The granules and tablets were characterized for particle size analysis, flow properties, tablet hardness, friability, moisture content, dissolution study, disintegration time and stability study. All results were found to be within acceptable limits. Development of all formulation tablets were found as best fitted for an immediate release of Metformin hydrochloride, acetaminophen and ferrous ascorbate. MADG delivered a robust manufacturing process for generation of granules with excellent flowability. The tablets prepared using this method were found to show better content uniformity, good compactability and low friability. Use of this approach aids to lower the amount of excipients used to overcome physiochemical limitation of the drug substances and there side effects. Both drying and milling steps in wet granulation were not required for MADG process. MADG became a cost effective process which could lead to reduced total tablet size and also save time.

Research paper thumbnail of Biodegradable Porous Starch Spheres as a Novel Carrier for Enhancement of Dissolution Rate and Oral Bioavailability of Itraconazole

Current Drug Delivery, 2017

A biodegradable porous starch (BPS) was developed in order to improve dissolution and oral bioava... more A biodegradable porous starch (BPS) was developed in order to improve dissolution and oral bioavailability of Itraconazole as a poorly water-soluble antifungal drug. BPS was developed by converting native starch from hydrogel to alcogel by solvent exchange method. The developed BPS carrier was characterized by SEM and nitrogen adsorption/desorption analysis to understand surface morphology and porosity distribution respectively. Itraconazole (ITR) was loaded on BPS by adsorption mediated solvent evaporation method, which provides a hydrophilic matrix powder. This causes drug distribution within hydrophilic matrix of porous starch. Solid-state characterization of optimized batch (ITR/BPS-3) was performed using DSC, PXRD, FTIR, SEM and FTIR imaging. In vitro dissolution and in vivo pharmacokinetic studies were performed to evaluate therapeutic potential of ITR/BPS-3 system. In vitro studies of ITR: BPS-3 system revealed a burst effect in drug release (100%) compared to marketed product, which showed (93%) drug release at end of 60 min. Moreover, ITR/BPS-3 system showed improved oral bioavailability up to 3.93 fold and marketed product shows 3.12 fold compared to ITR. This effect is due to high surface area, improved wettability and reduced crystallinity of ITR due to its adsorption into BPS. A successful methodology was reported to prepare BPS from raw starch.

Research paper thumbnail of Crosslinked Porous Starch Particles--a Promising Carrier

Polimery w medycynie

Background. Starch is one of the most potential natural polymers used for various bio application... more Background. Starch is one of the most potential natural polymers used for various bio applications. Literature reports a num- ber of modification strategies such as physical, chemical, enzymatic and genetic to enhance the positive attributes and iron out the undesired features of neat starch. To synthesize a crosslinked porous starch (CPS) as an efficient cargo for the delivery of calcium carbonate in an efficiently controlled manner for the treatment of hyperphosphatemia. The CPS carrier was synthesized using a natural crosslinker, malic acid. The drug delivery system was formulated, followed by the in situ loading of calcium carbonate during the preparation of the CPS. The developed system was characterized with respect to FTIR, DSC, SEM, moisture content, zeta potential, encapsulation efficiency, phosphate binding efficiency and dissolution studies. The developed formulation was observed to deliver calcium carbonate in an enterically controlled manner. The binding of calcium to p...

Research paper thumbnail of Exploring the potential of porous silicas as a carrier system for dissolution rate enhancement of artemether

Asian Journal of Pharmaceutical Sciences, 2016

Research paper thumbnail of Solubility and dissolution enhancement of efavirenz hot melt extruded amorphous solid dispersions using combination of polymeric blends: A QbD approach

European Journal of Pharmaceutical Sciences, 2016

Efavirenz is a non-nucleoside reverse transcriptase inhibitor and categorized in to BCS class II ... more Efavirenz is a non-nucleoside reverse transcriptase inhibitor and categorized in to BCS class II drug. The aim of the present investigation was to apply quality by design approach to enhance the solubility, dissolution and stability of amorphous solid dispersions (ASDs) of efavirenz using a combination of Soluplus® and HPMCAS-HF polymers. In design of experiments, the user defined quadratic model was used to study the effect of variable concentrations of Soluplus® and HPMCAS-HF for the formation of ASDs of efavirenz. Similarly, a prototype ASD was made using Soluplus® as a carrier with efavirenz loading of 30%. The efavirenz ASDs granular extrudates were evaluated for saturation solubility as well as dissolution rate studies. X-ray powder diffraction, Differential scanning calorimetry, Fourier transform infrared, Atomic force microscopy and FTIR imaging to determine the solid state of efavirenz in the ASDs. DSC and XRD data confirmed that bulk crystalline efavirenz transformed to the amorphous form during the hot melt extrusion processing. Prototype ASD batch showed instability upon storage as per ICH guidelines over a period of 6months, observations inferred from DSC, XRD and in vitro dissolution studies. The maximum dissolution rate was observed when Soluplus® and HPMCAS-HF was in ratio of (60:20) as optimized by design of experiments study. Moreover, the optimized ASDs batch were stable at 40°C, 75% RH for a period of 6months without any dissolution rate changes, and remained into amorphous state.