Swelling and drug release behavior of metformin HCl-loaded tamarind seed polysaccharide-alginate beads.

The paper describes the preparation, characterization, in vitro swelling and in vitro drug release of metformin HCl-loaded tamarind seed polysaccharide (TSP)-alginate beads were prepared by ionotropic-gelation technique and using CaCl2 as cross-linker. The prepared beads exhibited 32.73 ± 1.41% of drug loading (%), 94.86 ± 3.92% of drug encapsulation efficiency (%), and 1.24 ± 0.07 mm of average bead size. The bead surface morphology was analyzed by SEM. The drug-polymer interaction in the bead matrix was analyzed by FTIR analyses. These metformin HCl-loaded ionotropically gelled TSP-alginate beads demonstrated sustained in vitro drug release profile over 10h. These in vitro drug release exhibited pH-dependent drug release behavior. The in vitro drug release from these metformin HCl-loaded beads followed controlled-release (zero-order) pattern with super case-II transport mechanism. The swelling and degradation of these metformin HCl-loaded polymeric beads were found to be influenced by the pH of test mediums.

Screening of polysaccharides from tamarind, fenugreek and jackfruit seeds as pharmaceutical excipients.

The paper describes the isolation and screening of plant polysaccharides namely tamarind seed polysaccharide (TSP), fenugreek seed mucilage (FSM) and jackfruit seed starch (JFSS) from tamarind (Tamarindus indica L.) seeds, fenugreek (Trigonella foenum-graecum L.) seeds and jackfruit (Artocarpus heterophyllus L.) seeds, respectively. The yields of isolated dried TSP, FSM and JFSS were 47.00%, 17.36% and 18.86%, respectively. Various physicochemical properties like colour, odour, taste, solubility in water, pH and viscosity of these isolated plant polysaccharides were assessed. Isolated polysaccharide samples were subjected to some phytochemical identification tests. FTIR and (1)H NMR analyses of isolated polysaccharides were performed, which suggest the presence of sugar residues. Isolated TSP, FSM and JFSS can be used as pharmaceutical excipients in various pharmaceutical formulations.

Ispaghula mucilage-gellan mucoadhesive beads of metformin HCl: development by response surface methodology.

Response surface methodology based on 3(2) factorial design was used to develop ispaghula (Plantago ovata F.) husk mucilage (IHM)-gellan gum (GG) mucoadhesive beads containing metformin HCl through Ca(2+)-ion cross-linked ionotropic-gelation technique for the use in oral drug delivery. GG to IHM ratio and cross-linker (CaCl2) concentration were investigated as independent variables. Drug encapsulation efficiency (DEE, %) and cumulative drug release after 10h (R10h, %) were analyzed as dependent variables. The optimized mucoadhesive beads (F-O) showed DEE of 94.24 ± 4.18%, R10h of 59.13 ± 2.27%. These beads were also characterized by SEM and FTIR analyses. The in vitro drug release from these beads showed controlled-release (zero-order) pattern with super case-II transport mechanism over 10h. The optimized beads showed pH-dependent swelling and good mucoadhesivity with the goat intestinal mucosa. The optimized IHM-GG mucoadhesive beads containing metformin HCl exhibited significant antidiabetic effect in alloxan-induced diabetic rats over 10h.

Development of pectinate-ispagula mucilage mucoadhesive beads of metformin HCl by central composite design.

Ionotropically-gelled mucoadhesive beads of metformin HCl composed of low methoxy (LM) pectin-ispaghula husk mucilage (IHM) polymer-blend was developed and optimized using central composite design (spherical type, single center point, and α=1.414). Effects of LM pectin and IHM amounts on drug encapsulation efficiency (DEE) and cumulative drug release at 10h (R10h) were analysed using response surface methodology. The optimized beads containing metformin HCl (F-O) showed DEE of 86.98 ± 3.26% and R10h of 47.20 ± 1.28%. All these beads exhibited suitable controlled in vitro sustained drug release pattern with super case-II transport mechanism over 10h. These beads were also characterized by SEM and FTIR. The optimized beads also exhibited pH-dependent swelling, good mucoadhesivity with goat intestinal mucosa and significant hypoglycemic effect in alloxan-induced diabetic rats over prolonged period after oral administration, which could possibly be lucrative in terms of prolonged systemic absorption of metformin HCl maintaining tight blood glucose level and advanced patient compliance.

Tamarind seed polysaccharide-gellan mucoadhesive beads for controlled release of metformin HCl.

The paper describes the development, optimization and evaluation of tamarind seed polysaccharide (TSP)-blended gellan gum (GG) mucoadhesive beads containing metformin HCl through Ca(2+)-ion cross-linked ionic gelation for oral drug delivery. Effects of GG to TSP ratio and cross-linker (CaCl2) concentration on the drug encapsulation efficiency (DEE, %), and cumulative drug release after 10h (R10h, %) of TSP-GG mucoadhesive beads containing metformin HCl were optimized by 32 factorial design. The optimized mucoadhesive beads (F-O) showed DEE of 95.73 ± 4.02%, R10h of 61.22 ± 3.44% and mean diameter of 1.70 ± 0.24 mm.These beads were characterized by SEM and FTIR analyses. The in vitro drug release from these beads showed controlled-release (zero-order) pattern over a period of 10h.The optimized TSP-GG mucoadhesive beads also exhibited pH-dependent swelling, good mucoadhesivity with biological mucosal membrane and significant hypoglycemic effect in alloxan-induced diabetic rats over prolonged period after oral administration.

Artocarpus heterophyllus L. seed starch-blended gellan gum mucoadhesive beads of metformin HCl.

Jackfruit (Artocarpus heterophyllus Lam., family: Moraceae) seed starch (JFSS)-gellan gum (GG) mucoadhesive beads containing metformin HCl were developed through ionotropic gelation technique. The effect of GG to JFSS ratio and CaCl2 concentration on the drug encapsulation efficiency (DEE, %) and cumulative drug release at 10h (R10h, %) was optimized and analyzed using response surface methodology based on 3(2) factorial design. The optimized JFSS-GG beads containing metformin HCl showed DEE of 92.67±4.46%, R10h of 61.30±2.37%, and mean diameter of 1.67±0.27 mm. The optimized beads showed pH-dependent swelling and mucoadhesivity with the goat intestinal mucosa. The in vitro drug release from all these JFSS-GG beads containing metformin HCl was followed zero-order pattern (R(2)=0.9907-0.9975) with super case-II transport mechanism over a period of 10 h. The beads were also characterized by SEM and FTIR. The optimized JFSS-GG beads containing metformin HCl exhibited significant hypoglycemic effect in alloxan-induced diabetic rats over prolonged period after oral administration.

Development of calcium pectinate-tamarind seed polysaccharide mucoadhesive beads containing metformin HCl.

Novel mucoadhesive beads containing metformin HCl made of low methoxy (LM) pectin-tamarind seed polysaccharide (TSP) polymer-blend was developed through ionotropic-gelation technique and optimized using 3(2) factorial design. Effects of LM pectin and TSP amounts on drug encapsulation efficiency (DEE), and cumulative drug release at 10h (R10h) were analyzed using response surface methodology. The optimized calcium pectinate-TSP beads containing metformin HCl showed DEE of 95.12 ± 4.26%, R10h of 46.53 ± 3.28%, and mean diameter of 1.93 ± 0.26 mm. The in vitro drug release from these beads was followed controlled-release (zero-order) pattern with super case-II transport mechanism. These beads were also characterized by SEM and FTIR. The optimized beads also exhibited pH-dependent swelling, good mucoadhesivity with goat intestinal mucosa and significant hypoglycemic effect in alloxan-induced diabetic rats over prolonged period after oral administration.

Plantago ovata F. Mucilage-Alginate Mucoadhesive Beads for Controlled Release of Glibenclamide: Development, Optimization, and In Vitro-In Vivo Evaluation.

The current study deals with the development and optimization of ispaghula (Plantago ovata F.) husk mucilage- (IHM-) alginate mucoadhesive beads containing glibenclamide by ionotropic gelation technique. The effects of sodium alginate (SA) to IHM and cross-linker (CaCl2) concentration on the drug encapsulation efficiency (DEE, %), as well as cumulative drug release after 10 hours (R10 h, %), were optimized using 3(2) factorial design based on response surface methodology. The observed responses were coincided well with the predicted values by the experimental design. The optimized mucoadhesive beads exhibited 94.43 ± 4.80% w/w of DEE and good mucoadhesivity with the biological membrane in wash-off test and sustained drug release profile over 10 hours. The beads were also characterized by SEM and FTIR analyses. The in vitro drug release from these beads was followed by controlled release (zero-order) pattern with super case-II transport mechanism. The optimized glibenclamide-loaded IHM-alginate mucoadhesive beads showed significant antidiabetic effect in alloxan-induced diabetic rats over prolonged period after oral administration.

Development of biodegradable polymer based tamoxifen citrate loaded nanoparticles and effect of some manufacturing process parameters on them: a physicochemical and in-vitro evaluation.

The aim of the present study was to develop nanoparticles of tamoxifen citrate, a non-steroidal antiestrogenic drug used for the treatment of breast cancer. Biodegradable poly (D, L- lactide-co-glycolide)-85:15 (PLGA) was used to develop nanoparticles of tamoxifen citrate by multiple emulsification (w/o/w) and solvent evaporation technique. Drug-polymer ratio, polyvinyl alcohol concentrations, and homogenizing speeds were varied at different stages of preparation to optimize the desired size and release profile of drug. The characterization of particle morphology and shape was performed by field emission scanning electron microscope (FE-SEM) and particle size distribution patterns were studied by direct light scattering method using zeta sizer. In vitro drug release study showed that release profile of tamoxifen from biodegradable nanoparticles varied due to the change in speed of centrifugation for separation. Drug loading efficiency varied from 18.60% to 71.98%. The FE-SEM study showed that biodegradable nanoparticles were smooth and spherical in shape. The stability studies of tamoxifen citrate in the experimental nanoparticles showed the structural integrity of tamoxifen citrate in PLGA nanoparticles up to 60°C in the tested temperatures. Nanoparticles containing tamoxifen citrate could be useful for the controlled delivery of the drug for a prolonged period.

Preparation, characterization and in-vitro evaluation of sustained release protein-loaded nanoparticles based on biodegradable polymers.

Controlled drug delivery technology of proteins/peptides from biodegradable nanoparticles has emerged as one of the eminent areas to overcome formulation associated problems of the macromolecules. The purpose of the present investigation was to develop protein-loaded nanoparticles using biodegradable polymer poly L-lactide-co-glycolidic acid (PLGA) with bovine serum albumin (BSA) as a model protein. Despite many studies available with PLGA-based protein-loaded nanoparticles, production know-how, process parameters, protein loading, duration of protein release, narrowing polydispersity of particles have not been investigated enough to scale up manufacturing of protein-loaded nanoparticles in formulations. Different process parameters such as protein/polymer ratio, homogenizing speed during emulsifications, particle surface morphology and surface charges, particle size analysis and in-vitro protein release were investigated. The in-vitro protein release study suggests that release profile of BSA from nanoparticles could be modulated by changing protein-polymer ratios and/or by varying homogenizing speed during multiple-emulsion preparation technique. The formulation prepared with protein-polymer ratio of 1:60 at 17,500 rpm gave maximum protein-loading, minimum polydispersion with maximally sustained protein release pattern, among the prepared formulations. Decreased (10,000 rpm) or enhanced (24,000 rpm) homogenizing speeds resulted in increased polydispersion with larger particles having no better protein-loading and -release profiles in the present study.