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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., (Copyright © 2015 Elsevier B.V. All rights reserved.)

A novel dual crosslinked low-methoxyl (LM) pectinate-sterculia gum (SG) interpenetrating polymer network (IPN) beads was developed for intragastric ziprasidone delivery. The IPN beads were accomplished by simultaneous ionotropic gelation with zinc acetate and covalent crosslinking with glutaraldehyde. The effects of pectin and SG contents on drug entrapment efficiency (DEE, %), and cumulative drug release after 8h (Q8, %) were studied to optimize the IPN beads using a 3(2) factorial design. The optimized beads encapsulating ziprasidone HCl (F-O) displayed DEE of 87.98±1.15% and Q8 of 58.81±1.50% with excellent buoyancy (floating lag time <2min, % buoyancy at 8h >63%) and good mucoadhesivity with the goat gastric mucosa. In most cases, the drug release behaviour obeyed Higuchi kinetics with anomalous transport mechanism. The Zn-pectinate-SG IPN beads were also characterized by SEM, FTIR, DSC and P-XRD analyses., (Copyright © 2015 Elsevier Ltd. All rights reserved.)

Novel floating-mucoadhesive oil-entrapped alginate beads coated with crossslinked alginate-sterculia gum gel membrane was developed for gastroretentive risperidone delivery. Oil-entrapped alginate beads containing risperidone as core were prepared by ionotropic gelation technique. Effects of polymer to drug ratio and oil to water ratio on drug entrapment efficiency (%) and cumulative drug release after 8h (%) were studied to optimize the core beads by a 3(2) factorial design. The optimized beads (F-O) demonstrated drug entrapment efficiency of 83.73±0.81% and cumulative drug release of 70.84±0.27% after 8h. The biopolymeric-coated optimized beads exhibited excellent buoyancy, better ex vivo mucoadhesion and slower drug release rate. The drug release profiles of risperidone-loaded uncoated and coated beads were best fitted in Korsmeyer-Peppas model with Fickian diffusion mechanism. The beads were also examined for the drug-excipients compatibility, drug crystallinity and surface morphology by FTIR, P-XRD and SEM analyses, respectively., (Copyright © 2014 Elsevier Ltd. All rights reserved.)

A novel alginate gel-coated oil-entrapped calcium-alginate-tamarind gum (TG)-magnesium stearate (MS) composite floating beads was developed for intragastric risperidone delivery with a view to improving its oral bioavailability. The TG-blended alginate core beads containing olive oil and MS as low-density materials were accomplished by ionotropic gelation technique. Effects of polymer-blend ratio (sodium alginate:TG) and crosslinker (CaCl2) concentration on drug entrapment efficiency (DEE, %) and cumulative drug release after 8 h (Q8h, %) were studied to optimize the core beads by a 3(2) factorial design. The optimized beads (F-O) exhibited DEE of 75.19±0.75% and Q8h of 78.04±0.38% with minimum errors in prediction. The alginate gel-coated optimized beads displayed superior buoyancy and sustained drug release property. The drug release profiles of the drug-loaded uncoated and coated beads were best fitted in Higuchi kinetic model with Fickian and anomalous diffusion driven mechanisms, respectively. The optimized beads yielded a notable sustained drug release profile as compared to marketed immediate release preparation. The uncoated and coated Ca-alginate-TG-MS beads were also characterized by SEM, FTIR and P-XRD analyses. Thus, the newly developed alginate-gel coated oil-entrapped alginate-TG-MS composite beads are suitable for intragastric delivery of risperidone over a prolonged period of time., (Copyright © 2015 Elsevier B.V. All rights reserved.)

The utility of isolated okra (Hibiscus esculentus) gum (OG) was evaluated as a potential sustained drug release polymer-blends with sodium alginate in the development of controlled glibenclamide release ionically-gelled beads for oral use. OG was isolated from okra fruits and its solubility, pH, viscosity and moisture content were studied. Glibenclamide-loaded OG-alginate blend beads were prepared using CaCl2 as cross-linking agent through ionic-gelation technique. These ionically gelled beads showed drug entrapment efficiency of 64.19 ± 2.02 to 91.86 ± 3.24%. The bead sizes were within 1.12 ± 0.11 to 1.28 ± 0.15 mm. These glibenclamide-loaded OG-alginate blend beads exhibited sustained in vitro drug release over a prolonged period of 8 h. The in vitro drug release from these OG-alginate beads were followed controlled-release (zero-order) pattern with super case-II transport mechanism. The beads were also characterized by SEM and FTIR. The swelling and degradation of these beads was influenced by the pH of the test medium. These beads also exhibited good mucoadhesivity with goat intestinal mucosa.

Isoxsuprine HCl-loaded microbeads using sodium alginate (SA)-carboxymethyl cashew gum (CMCG) polymer-blends were developed through ionotropic-gelation technique using ZnSO4 as cross-linker. Effects of polymer-blend ratio and cross-linker concentration on drug encapsulation efficiency (DEE) and cumulative drug release at 7 h (R7 h) were optimized by 3(2) factorial design. Optimized microbeads were of excellent combination of high DEE (79.92±2.51%) and suitable sustained drug release pattern over a prolonged period of 7 h (58.67±2.26%). The microbead surface morphology was analyzed by SEM. The physical state of isoxsuprine HCl within the optimized microbead matrix was analyzed by FTIR and DSC. In vitro isoxsuprine HCl release from alginate-CMCG microbeads in phosphate buffer (pH, 6.8) showed prolonged sustained drug release and Korsmeyer-Peppas model (R2=0.9959-0.9992) over 7 h., (Copyright © 2014 Elsevier B.V. All rights reserved.)

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., (Copyright © 2014 Elsevier Ltd. All rights reserved.)

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., (Copyright © 2014 Elsevier B.V. All rights reserved.)

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., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

The paper describes development of aceclofenac-loaded pectinate-poly(vinyl pyrrolidone) [PVP] beads through ionotropic-gelation. Effects of amount of pectin and PVP on drug encapsulation efficiency (DEE), and cumulative drug release at 6h (R6h) were optimized by using response surface methodology. The optimized beads showed DEE of 96.58 ± 4.15% and R6h of 41.62 ± 2.18% with controlled drug release pattern. FTIR spectroscopy analysis revealed possible intermolecular hydrogen bonding, which could be formed between C=O groups of PVP and -OH groups of pectin in these beads. The swelling of these beads were influenced by pH of the medium., (Copyright © 2013 Elsevier B.V. All rights reserved.)

Aceclofenac-loaded alginate/gellan gum microspheres for prolonged aceclofenac release were prepared through maleic anhydride-induced unsaturated esterification. The drug entrapment efficiency of these microspheres was found 39.30 ± 1.28% to 98.46 ± 0.40% and their average particle sizes were 270-490 μm. These microspheres were characterized by FTIR, DSC, P-XRD and SEM analysis. The in vitro dissolution indicated prolonged sustained release of aceclofenac over 6h, which also followed the Korsmeyer-Peppas model (R(2)=0.9571-0.9952). The microspheres prepared through 3% (w/v) maleic anhydride-induced esterification exhibited comparatively slower drug-release. Most of the microspheres were followed Fickian diffusion mechanism except the microspheres containing higher gellan gum content, which followed anomalous (non-Fickian) diffusion. The in vivo results showed sustained systemic absorption of aceclofenac in rabbits and excellent anti-inflammatory activity in carrageenan-induced rats after oral administration over prolonged period., (Copyright © 2013 Elsevier B.V. All rights reserved.)

The work investigates the development and optimization of fenugreek (Trigonella foenum-graecum L.) seed mucilage (FSM)-alginate mucoadhesive beads containing metformin HCl through ionotropic gelation using 3(2) factorial design. The effect of polymer-blend ratio (sodium alginate to FSM) and cross-linker (CaCl(2)) concentration on the drug encapsulation efficiency (DEE, %), and cumulative drug release after 10h (R(10h), %) was optimized. The DEE (%) of all these beads was within the range of 71.63 ± 2.32 to 95.08 ± 3.73% with sustained in vitro drug release of 69.78 ± 2.43% to 95.70 ± 4.26% over 10h. The in vitro drug release from these beads was followed controlled-release (zero-order) pattern (R(2)=0.9910 to 0.9953) with super case-II transport mechanism. The average size of these beads was within the range of 0.92 ± 0.05 to 1.30 ± 0.14 mm. The beads were also characterized by SEM, FTIR and (1)H NMR. The swelling and degradation of FSM-alginate beads containing metformin HCl were influenced by pH of the test medium. These beads also exhibited good mucoadhesivity in wash-off test. The optimized FSM-alginate mucoadhesive beads containing metformin HCl showed significant hypoglycemic effect in alloxan-induced diabetic rats over prolonged period after oral administration., (Copyright © 2012 Elsevier B.V. All rights reserved.)

This work investigates the development, optimization and in vitro characterization of calcium alginate/gum Arabic beads by an ionotropic gelation method for prolonged sustained release of glibenclamide. The effects of amount of sodium alginate and gum Arabic as independent process variables on the drug encapsulation efficiency and drug release were optimized and analyzed based on central composite design and response surface methodology. Increment in drug encapsulation efficiency and decrease in drug release were found with the increase of both the amounts of sodium alginate and gum Arabic, used as polymer-blend. These optimized beads showed high drug encapsulation efficiency (86.02±2.97%), and suitable sustained drug release pattern over prolonged period (cumulative drug release after 7 h of 35.68±1.38%). The average size of these formulated dried beads containing glibenclamide ranged from 1.15±0.11 to 1.55±0.19 mm. The in vitro dissolution of these beads showed prolonged sustained release of glibenclamide over 7 h, which followed first-order model (R(2)=0.9886-0.9985) with anomalous (non-Fickian) diffusion mechanism (release exponent, n=0.72-0.81). The swelling and degradation of the optimized beads were influenced by pH of test mediums. These beads were also characterized by SEM and FTIR spectroscopy for surface morphology and excipients-drug interaction analysis, respectively. These developed calcium alginate/gum Arabic beads containing glibenclamide could possibly be advantageous in terms of advanced patient compliance with reduced dosing interval., (Copyright © 2012 Elsevier B.V. All rights reserved.)

Novel tamarind seed polysaccharide (TSP)-alginate mucoadhesive microspheres were prepared using TSP and alginate as blend in different ratios with different calcium chloride (CaCl(2)) concentration as a cross linker by ionotropic gelation. The prepared microspheres were of spherical shape having rough surfaces, and average particle sizes within the range of 752.12 ± 6.42 to 948.49 ± 20.92 µm. The drug entrapment efficiency of these microspheres were within the range between 58.12 ± 2.42 to 82.78 ± 3.43% w/w. Fourier transform infrared (FTIR) studies indicated that there were no reactions between gliclazide, and polymers (TSP, and sodium alginate) used. Different formulations of gliclazide loaded TSP-alginate microspheres showed prolonged in vitro release profiles of gliclazide over 12 hours in both stomach pH (pH 1.2), and intestinal pH (pH 7.4). It was found that the gliclazide release in gastric pH was comparatively slow and sustained than intestinal pH. These TSP-alginate microspheres also exhibited good mucoadhesivity. The in vivo studies on alloxan-induced diabetic rats (Animal Ethical Committee registration number: IFTM/837ac/0160) demonstrated the significant hypoglycemic effect of selected formulation of TSP-alginate mucoadhesive microspheres containing gliclazide on oral administration. This developed gliclazide loaded new TSP-alginate mucoadhesive microspheres may be very much useful for prolonged systemic absorption of gliclazide for proper maintaining blood glucose level and advanced patient compliance.

The present study deals with the development of novel pH-sensitive tamarind seed polysaccharide (TSP)-alginate composite beads for controlled diclofenac sodium delivery using response surface methodology by full 3(2) factorial design. The effect of polymer-blend ratio (sodium alginate:TSP) and cross-linker (CaCl(2)) concentration on the drug encapsulation efficiency (DEE, %) and drug release from diclofenac sodium loaded TSP-alginate composite beads prepared by ionotropic gelation was optimized. The observed responses were coincided well with the predicted values by the experimental design. The DEE (%) of these beads containing diclofenac sodium was within the range between 72.23±2.14 and 97.32±4.03% with sustained in vitro drug release (69.08±2.36-96.07±3.54% in 10 h). The in vitro drug release from TSP-alginate composite beads containing diclofenac sodium was followed by controlled-release pattern (zero-order kinetics) with case-II transport mechanism. Particle size range of these beads was 0.71±0.03-1.33±0.04 mm. The swelling and degradation of the developed beads were influenced by different pH of the test medium. The FTIR and NMR analyses confirmed the compatibility of the diclofenac sodium with TSP and sodium alginate used to prepare the diclofenac sodium loaded TSP-alginate composite beads. The newly developed TSP-alginate composite beads are suitable for controlled delivery of diclofenac sodium for prolonged period., (Copyright © 2011 Elsevier B.V. All rights reserved.)