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

Nayak AK, Pal D, Santra K - J Pharm (Cairo) (2013)

Bottom Line: 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 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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Jharpokharia, Mayurbhanj, Odisha 757086, India.

ABSTRACT
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.

No MeSH data available.


The overlay plot indicating the region of optimal process variable settings.
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4590812&req=5

fig10: The overlay plot indicating the region of optimal process variable settings.

Mentions: Numerical optimization technique using the desirability approach was employed to develop optimized formulations with desired response (optimum quality). The desirable ranges of the independable variables (factors) were restricted to 1.00 ≤ X1 ≤ 1.50 and 9.50 ≤ X2 ≤ 11.50, whereas the desirable ranges of responses were restricted to 95.00 ≤ DEE ≤ 100.00% and 60.00 ≤ R10 h ≤ 65.00%. The optimal values of responses were obtained by numerical analysis using the Design-Expert Version 8.0.6.1 software based on the criterion of desirability. The desirability plot indicating desirable regression ranges for optimal process variable settings was presented in Figure 9, and overlay plot indicating the region of optimal process variable settings was presented in Figure 10. In order to evaluate the optimization capability of these models generated according to the results of 32 factorial design, optimized glibenclamide-loaded IHM-alginate beads were prepared using one of the optimal process variable settings proposed by the design (prediction R2 = 1). The selected optimal process variable setting used for the formulation of optimized formulation was X1 = 1.35 and X2 = 10.99. The optimized beads containing glibenclamide (F-O) were evaluated for DEE  (%) and R10 h(%). Table 3 lists the results of experiments with predicted responses by the mathematical models and those actually observed. The optimized glibenclamide-loaded IHM-alginate beads (F-O) showed DEE of 94.43 ± 4.80% and R10 h of 65.78 ± 3.44% with small error values (0.94, and −3.69, resp.), indicating that mathematical models obtained from the 32 factorial design were fitted well.


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

Nayak AK, Pal D, Santra K - J Pharm (Cairo) (2013)

The overlay plot indicating the region of optimal process variable settings.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590812&req=5

fig10: The overlay plot indicating the region of optimal process variable settings.
Mentions: Numerical optimization technique using the desirability approach was employed to develop optimized formulations with desired response (optimum quality). The desirable ranges of the independable variables (factors) were restricted to 1.00 ≤ X1 ≤ 1.50 and 9.50 ≤ X2 ≤ 11.50, whereas the desirable ranges of responses were restricted to 95.00 ≤ DEE ≤ 100.00% and 60.00 ≤ R10 h ≤ 65.00%. The optimal values of responses were obtained by numerical analysis using the Design-Expert Version 8.0.6.1 software based on the criterion of desirability. The desirability plot indicating desirable regression ranges for optimal process variable settings was presented in Figure 9, and overlay plot indicating the region of optimal process variable settings was presented in Figure 10. In order to evaluate the optimization capability of these models generated according to the results of 32 factorial design, optimized glibenclamide-loaded IHM-alginate beads were prepared using one of the optimal process variable settings proposed by the design (prediction R2 = 1). The selected optimal process variable setting used for the formulation of optimized formulation was X1 = 1.35 and X2 = 10.99. The optimized beads containing glibenclamide (F-O) were evaluated for DEE  (%) and R10 h(%). Table 3 lists the results of experiments with predicted responses by the mathematical models and those actually observed. The optimized glibenclamide-loaded IHM-alginate beads (F-O) showed DEE of 94.43 ± 4.80% and R10 h of 65.78 ± 3.44% with small error values (0.94, and −3.69, resp.), indicating that mathematical models obtained from the 32 factorial design were fitted well.

Bottom Line: 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 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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Jharpokharia, Mayurbhanj, Odisha 757086, India.

ABSTRACT
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.

No MeSH data available.