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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.


Linear correlation plot relating R10 h(%) between the actual and the predicted values.
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fig3: Linear correlation plot relating R10 h(%) between the actual and the predicted values.

Mentions: Linear correlation plots between the actual, the predicted response variables are presented in Figures 1 and 2, and their corresponding residual plots showing the scatter of the residuals versus predicted values are presented in Figures 3 and 4. The influences of main effects (factors) on responses (here, DEE and R10 h) were further elucidated by response surface methodology. Response surface methodology is a widely proficient approach in the development and optimization of drug delivery devices [5, 8, 28]. Response surface methodology encompasses the generation of model equations of the investigated responses over the experimental domain to determine optimum formulation (s) [29]. The three-dimensional response surface plot is very useful in learning about the main and interaction effects of the independent variables (factors), whereas two-dimensional contour plot gives a visual representation of values of the response [5]. The three-dimensional response surface plot relating DEE (Figure 5) indicates the increment of DEE with the lowering of SA: IHM (X1) and increasing of CaCl2 concentration (X2). However, an increment in R10 h values with the increasing of SA: IHM (X1) and lowering of CaCl2 concentration (X2) is indicated by the three-dimensional response surface plot relating R10 h (Figure 6). All the two-dimensional contour plots relating measured responses (Figures 7 and 8) showed nonlinear relationships between independable variables, investigated for this study.


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)

Linear correlation plot relating R10 h(%) between the actual and the predicted values.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig3: Linear correlation plot relating R10 h(%) between the actual and the predicted values.
Mentions: Linear correlation plots between the actual, the predicted response variables are presented in Figures 1 and 2, and their corresponding residual plots showing the scatter of the residuals versus predicted values are presented in Figures 3 and 4. The influences of main effects (factors) on responses (here, DEE and R10 h) were further elucidated by response surface methodology. Response surface methodology is a widely proficient approach in the development and optimization of drug delivery devices [5, 8, 28]. Response surface methodology encompasses the generation of model equations of the investigated responses over the experimental domain to determine optimum formulation (s) [29]. The three-dimensional response surface plot is very useful in learning about the main and interaction effects of the independent variables (factors), whereas two-dimensional contour plot gives a visual representation of values of the response [5]. The three-dimensional response surface plot relating DEE (Figure 5) indicates the increment of DEE with the lowering of SA: IHM (X1) and increasing of CaCl2 concentration (X2). However, an increment in R10 h values with the increasing of SA: IHM (X1) and lowering of CaCl2 concentration (X2) is indicated by the three-dimensional response surface plot relating R10 h (Figure 6). All the two-dimensional contour plots relating measured responses (Figures 7 and 8) showed nonlinear relationships between independable variables, investigated for this study.

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.