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Louis Cartilier - One of the best experts on this subject based on the ideXlab platform.
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High-amylose sodium carboxymethyl starch matrices for oral, Sustained Drug Release: development of a spray-drying manufacturing process.
Drug development and industrial pharmacy, 2010Co-Authors: F. Brouillet, Louis Cartilier, Gilles Baylac, Bernard BatailleAbstract:Context: High-amylose sodium carboxymethyl starch (HASCA) was recently proposed as a material for oral, Sustained Drug-Release tablets prepared by direct compression. It was produced on a pilot scale, but appeared to be unsuitable for tableting and Sustained Drug Release. Pilot-scale dry powder HASCA was dispersed in hot water and then precipitated with ethanol to give a dry powder presenting the required properties, but very high volumes of ethanol were used to recover the product. Objective: A process was therefore designed to transform totally amorphous pregelatinized HASCA by spray-drying into a suitable Sustained Drug-Release excipient for matrix tablets while decreasing ethanol quantities. Results and discussion: During the first manufacturing step, that is, heating of the initial hydro-alcoholic suspension, powder and water concentrations are key parameters for the acquisition of excellent binding properties. Hence, a variable ratio of amylose Vh, a crystalline polymorph of amylose, to the amorphous form, is observed depending on the key parameter values. As the most crystalline samples give the weakest tablets, binding properties do not appear to be linked to the presence of a Vh form of amylose. On the other hand, a high water concentration results in excessive tablet strength, that is, inverse conditions leading to the appearance of a Vh form of amylose. Finally, variations in hydro-alcoholic composition appear to affect only tableting properties and do not influence the Drug-Release rate. Conclusion: A process designed to transform totally amorphous pregelatinized HASCA by spray-drying is proposed for easier, economical industrial HASCA production.
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high amylose sodium carboxymethyl starch matrices for oral Sustained Drug Release formulation aspects and in vitro Drug Release evaluation
International Journal of Pharmaceutics, 2008Co-Authors: F. Brouillet, Bernard Bataille, Louis CartilierAbstract:Abstract High-amylose sodium carboxymethyl starch (HASCA), produced by spray-drying (SD), was previously shown to have interesting properties as a promising pharmaceutical Sustained Drug-Release tablet excipient for direct compression, including ease of manufacture and high crushing strength. This study describes the effects of some important formulation parameters, such as compression force (CF), tablet weight (TW), Drug-loading and electrolyte particle size, on acetaminophen-Release performances from Sustained Drug-Release matrix tablets based on HASCA. An interesting linear relationship between TW and Release time was observed for a typical formulation of the system consisting of 40% (w/w) acetaminophen as model Drug and 27.5% NaCl as model electrolyte dry-mixed with HASCA. Application of the Peppas and Sahlin model gave a better understanding of the mechanisms involved in Drug-Release from the HASCA matrix system, which is mainly controlled by surface gel layer formation. Indeed, augmenting TW increased the contribution of the diffusion mechanism. CFs ranging from 1 to 2.5 tonnes/cm2 had no significant influence on the Release properties of tablets weighing 400 or 600 mg. NaCl particle size did not affect the acetaminophen-Release profile. Finally, these results prove that the new SD process developed for HASCA manufacture is suitable for obtaining similar-quality HASCA in terms of Release and compression performances.
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High-amylose carboxymethyl starch matrices for oral Sustained Drug-Release: in vitro and in vivo evaluation.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 2006Co-Authors: Teresa Nabais, Caroline Chebli, F. Brouillet, Bernard Bataille, S. Kyriacos, Mohamad Mroueh, P. Amores Da Silva, Louis CartilierAbstract:Abstract High-amylose corn starch, that contains 70% of amylose chains and 30% of amylopectin, has been used to obtain substituted amylose (SA) polymers. Tablets have been prepared by direct compression, i.e. dry mixing of Drug and SA, followed by compression, which is the easiest way to manufacture an oral dosage form. Until now, their controlled-Release properties have been assessed only by an in vitro dissolution test. Amylose-based polymers are normally subject to biodegradation by α-amylase enzymes present in the gastrointestinal tract, but matrix systems show no significant degradation of tablets by α-amylase in vitro. High-amylose sodium carboxymethyl starch (HASCA) is an interesting excipient for Sustained Drug-Release in solid oral dosage forms. In addition to the easy manufacture of tablets by direct compression, the results show that in vitro Drug-Release from an optimized HASCA formulation is not affected by either acidic pH value or acidic medium residence time. In addition, a compressed blend of HASCA with an optimized quantity of sodium chloride provides a pharmaceutical Sustained-Release tablet with improved integrity for oral administration. In vivo studies demonstrate extended Drug absorption, showing that the matrix tablets do not disintegrate immediately. Nevertheless, acetaminophen does not seem to be the most appropriate Drug for this type of formulation.
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Effect of some physical parameters on the Sustained Drug-Release properties of substituted amylose matrices.
International Journal of Pharmaceutics, 2000Co-Authors: Caroline Chebli, Louis CartilierAbstract:Substituted amylose (SA) matrix Drug tablets prepared by direct compression show Sustained Drug-Release properties. The influence of compression force (CF) and tablet weight (TW) on Release properties was studied. CF ranging from 0.5 to 5.0 tons/cm2 has no significant effect on the Release properties of SA,G (glycidol) polymers, with a degree of substitution (DS) greater than 1.5. For a low DS, an augmentation of CF increases the Release time of acetaminophen, used as a model Drug, until a certain limit is reached. On the other hand, TW has a major effect on the Release time of acetaminophen. Release time is directly proportional to TW. The effect of the nature of the active material, its solubility and its concentration in the formulation on the Release properties of SA,G polymers was also evaluated, demonstrating the versatility of the system.
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Substituted amylose as a matrix for Sustained Drug Release.
Pharmaceutical research, 1999Co-Authors: Caroline Chebli, I Moussa, S Buczkowski, Louis CartilierAbstract:Amylose derivatives form an important group of polymers, and many of them can be used as Drug Sustained-Release systems. Substituted amylose can be prepared in a 1-step reaction with substituent(s) in a basic medium. The substituents can be represented as (A-R), where (A) serves an epoxy, halide or suitable organic or inorganic function reacting with hydroxyl groups located on the amylose chain, and (R) is an organic radical. The present work shows the synthesis of different polymers and the effect of different (A) and/or (R) and their different degrees of substitution (n) on the Sustained Drug Release from matrix tablets prepared by direct compression. SA polymers are interesting excipients for the preparation of controlled Drug Release tablets.
Ashim K. Mitra - One of the best experts on this subject based on the ideXlab platform.
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Thermosensitive hydrogel-based Drug delivery system for Sustained Drug Release
Journal of Polymer Research, 2019Co-Authors: Pratikkumar Patel, Abhirup Mandal, Vrinda Gote, Ashim K. MitraAbstract:Hydrogels are unique biomaterials that have demonstrated tremendous potential in sustaining Drug Release. Significant effort has been made to impart stimuli sensitivity and incorporate hydrophilic molecules in a stable hydrogel network. Although, thermosensitive hydrogels have exhibited promising interventions, formulation of a biodegradable, stable thermosensitive hydrogel for Sustained Drug Release remain to be vastly studied. Here, a novel micellarization strategy was exploited to achieve a biodegradable thermosensitive hydrogel with improved stability. Two triblock co-polymers, PCL-PEG-PCL (600–2000-600) and PCL-PEG-PCL (1000–2000-1000) with different physical properties were employed to achieve optimal critical gelling concentration and critical solution temperature (LCST) that can form a stable hydrogel network at body temperature. A library of triblock co-polymers were synthesized utilizing ε-caprolactone and poly ethylene glycol (PEG) of various chain lengths. The block co-polymers exhibiting desired physical properties were further characterized using NMR and GPC analytical techniques. Release study of diclofenac sodium was examined in presence of the thermosensitive hydrogel. The results indicated that the hydrogel Sustained the Release of diclofenac sodium by ~100-folds. Kinetic models further suggested a first order Release rate, indicating that the Release is primarily mediated by diffusion through porous membranes of the hydrogel. Such hydrogel based Drug delivery system promises an effective strategy for sustaining Drug Release for the treatment of diseases.
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Thermosensitive hydrogel-based Drug delivery system for Sustained Drug Release
Journal of Polymer Research, 2019Co-Authors: Pratikkumar Patel, Abhirup Mandal, Vrinda Gote, Dhananjay Pal, Ashim K. MitraAbstract:Hydrogels are unique biomaterials that have demonstrated tremendous potential in sustaining Drug Release. Significant effort has been made to impart stimuli sensitivity and incorporate hydrophilic molecules in a stable hydrogel network. Although, thermosensitive hydrogels have exhibited promising interventions, formulation of a biodegradable, stable thermosensitive hydrogel for Sustained Drug Release remain to be vastly studied. Here, a novel micellarization strategy was exploited to achieve a biodegradable thermosensitive hydrogel with improved stability. Two triblock co-polymers, PCL-PEG-PCL (600–2000-600) and PCL-PEG-PCL (1000–2000-1000) with different physical properties were employed to achieve optimal critical gelling concentration and critical solution temperature (LCST) that can form a stable hydrogel network at body temperature. A library of triblock co-polymers were synthesized utilizing e-caprolactone and poly ethylene glycol (PEG) of various chain lengths. The block co-polymers exhibiting desired physical properties were further characterized using NMR and GPC analytical techniques. Release study of diclofenac sodium was examined in presence of the thermosensitive hydrogel. The results indicated that the hydrogel Sustained the Release of diclofenac sodium by ~100-folds. Kinetic models further suggested a first order Release rate, indicating that the Release is primarily mediated by diffusion through porous membranes of the hydrogel. Such hydrogel based Drug delivery system promises an effective strategy for sustaining Drug Release for the treatment of diseases.
Bernard Bataille - One of the best experts on this subject based on the ideXlab platform.
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High-amylose sodium carboxymethyl starch matrices for oral, Sustained Drug Release: development of a spray-drying manufacturing process.
Drug development and industrial pharmacy, 2010Co-Authors: F. Brouillet, Louis Cartilier, Gilles Baylac, Bernard BatailleAbstract:Context: High-amylose sodium carboxymethyl starch (HASCA) was recently proposed as a material for oral, Sustained Drug-Release tablets prepared by direct compression. It was produced on a pilot scale, but appeared to be unsuitable for tableting and Sustained Drug Release. Pilot-scale dry powder HASCA was dispersed in hot water and then precipitated with ethanol to give a dry powder presenting the required properties, but very high volumes of ethanol were used to recover the product. Objective: A process was therefore designed to transform totally amorphous pregelatinized HASCA by spray-drying into a suitable Sustained Drug-Release excipient for matrix tablets while decreasing ethanol quantities. Results and discussion: During the first manufacturing step, that is, heating of the initial hydro-alcoholic suspension, powder and water concentrations are key parameters for the acquisition of excellent binding properties. Hence, a variable ratio of amylose Vh, a crystalline polymorph of amylose, to the amorphous form, is observed depending on the key parameter values. As the most crystalline samples give the weakest tablets, binding properties do not appear to be linked to the presence of a Vh form of amylose. On the other hand, a high water concentration results in excessive tablet strength, that is, inverse conditions leading to the appearance of a Vh form of amylose. Finally, variations in hydro-alcoholic composition appear to affect only tableting properties and do not influence the Drug-Release rate. Conclusion: A process designed to transform totally amorphous pregelatinized HASCA by spray-drying is proposed for easier, economical industrial HASCA production.
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high amylose sodium carboxymethyl starch matrices for oral Sustained Drug Release formulation aspects and in vitro Drug Release evaluation
International Journal of Pharmaceutics, 2008Co-Authors: F. Brouillet, Bernard Bataille, Louis CartilierAbstract:Abstract High-amylose sodium carboxymethyl starch (HASCA), produced by spray-drying (SD), was previously shown to have interesting properties as a promising pharmaceutical Sustained Drug-Release tablet excipient for direct compression, including ease of manufacture and high crushing strength. This study describes the effects of some important formulation parameters, such as compression force (CF), tablet weight (TW), Drug-loading and electrolyte particle size, on acetaminophen-Release performances from Sustained Drug-Release matrix tablets based on HASCA. An interesting linear relationship between TW and Release time was observed for a typical formulation of the system consisting of 40% (w/w) acetaminophen as model Drug and 27.5% NaCl as model electrolyte dry-mixed with HASCA. Application of the Peppas and Sahlin model gave a better understanding of the mechanisms involved in Drug-Release from the HASCA matrix system, which is mainly controlled by surface gel layer formation. Indeed, augmenting TW increased the contribution of the diffusion mechanism. CFs ranging from 1 to 2.5 tonnes/cm2 had no significant influence on the Release properties of tablets weighing 400 or 600 mg. NaCl particle size did not affect the acetaminophen-Release profile. Finally, these results prove that the new SD process developed for HASCA manufacture is suitable for obtaining similar-quality HASCA in terms of Release and compression performances.
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High-amylose carboxymethyl starch matrices for oral Sustained Drug-Release: in vitro and in vivo evaluation.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 2006Co-Authors: Teresa Nabais, Caroline Chebli, F. Brouillet, Bernard Bataille, S. Kyriacos, Mohamad Mroueh, P. Amores Da Silva, Louis CartilierAbstract:Abstract High-amylose corn starch, that contains 70% of amylose chains and 30% of amylopectin, has been used to obtain substituted amylose (SA) polymers. Tablets have been prepared by direct compression, i.e. dry mixing of Drug and SA, followed by compression, which is the easiest way to manufacture an oral dosage form. Until now, their controlled-Release properties have been assessed only by an in vitro dissolution test. Amylose-based polymers are normally subject to biodegradation by α-amylase enzymes present in the gastrointestinal tract, but matrix systems show no significant degradation of tablets by α-amylase in vitro. High-amylose sodium carboxymethyl starch (HASCA) is an interesting excipient for Sustained Drug-Release in solid oral dosage forms. In addition to the easy manufacture of tablets by direct compression, the results show that in vitro Drug-Release from an optimized HASCA formulation is not affected by either acidic pH value or acidic medium residence time. In addition, a compressed blend of HASCA with an optimized quantity of sodium chloride provides a pharmaceutical Sustained-Release tablet with improved integrity for oral administration. In vivo studies demonstrate extended Drug absorption, showing that the matrix tablets do not disintegrate immediately. Nevertheless, acetaminophen does not seem to be the most appropriate Drug for this type of formulation.
Pratikkumar Patel - One of the best experts on this subject based on the ideXlab platform.
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Thermosensitive hydrogel-based Drug delivery system for Sustained Drug Release
Journal of Polymer Research, 2019Co-Authors: Pratikkumar Patel, Abhirup Mandal, Vrinda Gote, Ashim K. MitraAbstract:Hydrogels are unique biomaterials that have demonstrated tremendous potential in sustaining Drug Release. Significant effort has been made to impart stimuli sensitivity and incorporate hydrophilic molecules in a stable hydrogel network. Although, thermosensitive hydrogels have exhibited promising interventions, formulation of a biodegradable, stable thermosensitive hydrogel for Sustained Drug Release remain to be vastly studied. Here, a novel micellarization strategy was exploited to achieve a biodegradable thermosensitive hydrogel with improved stability. Two triblock co-polymers, PCL-PEG-PCL (600–2000-600) and PCL-PEG-PCL (1000–2000-1000) with different physical properties were employed to achieve optimal critical gelling concentration and critical solution temperature (LCST) that can form a stable hydrogel network at body temperature. A library of triblock co-polymers were synthesized utilizing ε-caprolactone and poly ethylene glycol (PEG) of various chain lengths. The block co-polymers exhibiting desired physical properties were further characterized using NMR and GPC analytical techniques. Release study of diclofenac sodium was examined in presence of the thermosensitive hydrogel. The results indicated that the hydrogel Sustained the Release of diclofenac sodium by ~100-folds. Kinetic models further suggested a first order Release rate, indicating that the Release is primarily mediated by diffusion through porous membranes of the hydrogel. Such hydrogel based Drug delivery system promises an effective strategy for sustaining Drug Release for the treatment of diseases.
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Thermosensitive hydrogel-based Drug delivery system for Sustained Drug Release
Journal of Polymer Research, 2019Co-Authors: Pratikkumar Patel, Abhirup Mandal, Vrinda Gote, Dhananjay Pal, Ashim K. MitraAbstract:Hydrogels are unique biomaterials that have demonstrated tremendous potential in sustaining Drug Release. Significant effort has been made to impart stimuli sensitivity and incorporate hydrophilic molecules in a stable hydrogel network. Although, thermosensitive hydrogels have exhibited promising interventions, formulation of a biodegradable, stable thermosensitive hydrogel for Sustained Drug Release remain to be vastly studied. Here, a novel micellarization strategy was exploited to achieve a biodegradable thermosensitive hydrogel with improved stability. Two triblock co-polymers, PCL-PEG-PCL (600–2000-600) and PCL-PEG-PCL (1000–2000-1000) with different physical properties were employed to achieve optimal critical gelling concentration and critical solution temperature (LCST) that can form a stable hydrogel network at body temperature. A library of triblock co-polymers were synthesized utilizing e-caprolactone and poly ethylene glycol (PEG) of various chain lengths. The block co-polymers exhibiting desired physical properties were further characterized using NMR and GPC analytical techniques. Release study of diclofenac sodium was examined in presence of the thermosensitive hydrogel. The results indicated that the hydrogel Sustained the Release of diclofenac sodium by ~100-folds. Kinetic models further suggested a first order Release rate, indicating that the Release is primarily mediated by diffusion through porous membranes of the hydrogel. Such hydrogel based Drug delivery system promises an effective strategy for sustaining Drug Release for the treatment of diseases.
Amit Kumar Nayak - One of the best experts on this subject based on the ideXlab platform.
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Ionotropically gelled alginate particles in Sustained Drug Release
Alginates in Drug Delivery, 2020Co-Authors: Amit Kumar Nayak, Saquib HasnainAbstract:Abstract Since the past few decades, the preparation of polymeric particles as multiple-unit Sustained Drug releasing carriers like beads, microparticles, and nanoparticles, via the ionotropic gelation technique, is being expanded as a fashionable biopolymer research, especially in the biomedical areas including Drug delivery applications. Ionotropically gelled different biopolymeric particles are synthesized employing one or more than one ionic natured polymer(s). Most of the reported ionotropically gelled Drug releasing systems was composed of anioinic polymers like sodium alginate, low methoxy pectin, gellan gum, and sodium carboxymethyl cellulose and cationic polymer like chitosan. Among these, alginates have extensively utilized for the preparation of biopolymeric beads, microparticles, nanoparticles, etc. via the ionotropic gelation employing various trivalent as well as divalent metal cations (e.g., Al3+, Fe3+, Ca2+, Cu2+, Zn2+, Cd2+, Ba2+, Pb2+). A variety of Drug candidates have successfully been encapsulated within ionotropically gelled alginate-based particles and thereby, these Drug encapsulated particles have been demonstrated diverse profiles of Drug releasing in Sustained manner over a longer period. The current chapter deals with a useful discussion on various ionotropically gelled alginate-based particles for Sustained Drug releasing.
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Alginate-based interpenetrating polymer networks for Sustained Drug Release
Alginates in Drug Delivery, 2020Co-Authors: Saquib Hasnain, Priyanka Ray, Amit Kumar NayakAbstract:Abstract In the biomaterial research, especially in the biopolymeric field, the designing of numerous interpenetrating polymeric networking (IPN) systems has already unlocked innovative opportunities. IPN systems are made of at least two polymers or more. In general, IPN systems are prepared when a minimum single polymeric networking is synthesized with the instantaneous occurrence of other polymer(s). The mechanical characteristics as well as the phase stabilities of the end products are enhanced in terms of desired quality via the formations of IPNs, which directs the extensive industrial applications of these IPNs. During the past few decades, several natural polysaccharidic polymers have already been tested and used in the preparations and evaluations of many IPN systems for Sustained Drug-releasing applications. Alginates belong to the group of naturally occurring anionic polysaccharides and have extensively been exploited to develop numerous alginate-based IPNs for Drug delivery. In the current chapter, the recent literature on various alginate-based IPNs for Sustained Release of Drug delivery has been reviewed. First, IPNs and their classifications of IPNs have been discussed. Afterward, the sources, general properties, and the need for modifications of alginate have been discussed. Finally, the recent researches that extensively synthesized and evaluated the use of various alginate-based IPNs for Sustained releasing Drug delivery have been summarized.
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Gelled Microparticles/Beads of Sterculia Gum and Tamarind Gum for Sustained Drug Release
Polymer Gels, 2018Co-Authors: Amit Kumar Nayak, M. Saquib Hasnain, Dilipkumar PalAbstract:In recent years, a variety of biocompatible natural polysaccharides are extensively investigated as pharmaceutical excipients in designing various pharmaceutical formulations. Among these, sterculia gum and tamarind gum have emerged as two popular biopolymer candidates, which have found their applications in designing of various Sustained Drug releasing dosage forms. Presently, both sterculia gum and tamarind gum have been employed to design oral multiple unit Sustained Release systems such as microparticles, beads. The present chapter deals with a helpful and comprehensive discussion on already reported different microparticles/beads made of sterculia gum and tamarind gum, which have shown a promise in Sustained Drug releasing capacity over a longer period after oral administration. This chapter will be helpful in applying appropriate strategies or achieving desired controlled Sustained Drug Release profiles from microparticles/beads made of sterculia gum and tamarind gum.
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gelled microparticles beads of sterculia gum and tamarind gum for Sustained Drug Release
2018Co-Authors: Amit Kumar Nayak, Saquib M Hasnain, Dilipkumar PalAbstract:In recent years, a variety of biocompatible natural polysaccharides are extensively investigated as pharmaceutical excipients in designing various pharmaceutical formulations. Among these, sterculia gum and tamarind gum have emerged as two popular biopolymer candidates, which have found their applications in designing of various Sustained Drug releasing dosage forms. Presently, both sterculia gum and tamarind gum have been employed to design oral multiple unit Sustained Release systems such as microparticles, beads. The present chapter deals with a helpful and comprehensive discussion on already reported different microparticles/beads made of sterculia gum and tamarind gum, which have shown a promise in Sustained Drug releasing capacity over a longer period after oral administration. This chapter will be helpful in applying appropriate strategies or achieving desired controlled Sustained Drug Release profiles from microparticles/beads made of sterculia gum and tamarind gum.
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Alginate-based bipolymeric-nanobioceramic composite matrices for Sustained Drug Release.
International journal of biological macromolecules, 2015Co-Authors: M. Saquib Hasnain, Amit Kumar Nayak, Mukul Singh, Mohammad Tabish, Mohammed Tahir Ansari, Tahseen Jahan AraAbstract:Alginate-based bipolymeric-nanobioceramic composite matrices for Sustained Drug Release were developed through incorporation of nano-hydroxyapatite [nHAp] powders within ionotropically-gelled calcium ion-induced alginate-poly (vinyl pyrrolidone) blends polymeric systems. nHAp powders were synthesized by precipitation technique using calcium hydroxide [Ca(OH)2] and orthophosphoric acid [H3PO4] as raw materials. The average particle size of these was synthesized. nHAp powders was found as 19.04 nm and used to prepare nHAp-alginate-PVP beads containing DS. These beads exhibited Drug entrapment efficiency (%) of 65.82±1.88 to 94.45±3.72% and average bead sizes of 0.98±0.07 to 1.23±0.15 mm. These beads were characterized by scanning electron microscopy (SEM) and Fourier transform-infra red (FTIR) spectroscopy analyses. Various nHAp-alginate-PVP beads containing DS exhibited prolonged Sustained Drug Release and followed the Koresmeyer-Peppas model of Drug Release (R2=0.9908-0.9978) with non-Fickian Release (anomalous transport) mechanism (n=0.73-0.84) for Drug Release over 8 h.
