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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.


Comparative in vivo mean percentage reduction in blood glucose level in alloxan-induced diabetic rats after oral administration of pure glibenclamide and optimized glibenclamide-loaded IHM-alginate mucoadhesive beads (F-O).
© Copyright Policy - open-access
Related In: Results  -  Collection


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fig16: Comparative in vivo mean percentage reduction in blood glucose level in alloxan-induced diabetic rats after oral administration of pure glibenclamide and optimized glibenclamide-loaded IHM-alginate mucoadhesive beads (F-O).

Mentions: In alloxan-induced diabetic rats, the comparative in vivo blood glucose level and the mean percentage reduction in blood glucose level after oral administration of pure glibenclamide and optimized glibenclamide-loaded IHM-alginate mucoadhesive beads (F-O) are presented in Figures 15 and 16, respectively. In case of the group treated with pure glibenclamide (Group A), a rapid reduction in blood glucose level was observed within 2-3 hours of administration, and after that, the blood glucose level recovered rapidly towards the normal level. In case of the group (Group B) treated with optimized glibenclamide-loaded IHM-alginate mucoadhesive beads, the reduction in blood glucose level was found slower than that of the group treated with pure glibenclamide (Group A) up to 3 hours. Significant differences (P < 0.05) were found between the blood glucose levels after administration of pure glibenclamide and optimized glibenclamide-loaded IHM-alginate mucoadhesive beads (F-O) at each time point measured. However, the reductions in glucose level were increased gradually with the increment of time in case of Group B (treated with optimized glibenclamide-loaded IHM-alginate mucoadhesive beads) and were sustained over 10 hours. A 25% reduction in glucose level is considered a significant hypoglycemic effect [29]. Therefore, the significant hypoglycemic effect by the optimized glibenclamide-loaded IHM-alginate mucoadhesive beads (F-O) was observed over 10 hours.


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)

Comparative in vivo mean percentage reduction in blood glucose level in alloxan-induced diabetic rats after oral administration of pure glibenclamide and optimized glibenclamide-loaded IHM-alginate mucoadhesive beads (F-O).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig16: Comparative in vivo mean percentage reduction in blood glucose level in alloxan-induced diabetic rats after oral administration of pure glibenclamide and optimized glibenclamide-loaded IHM-alginate mucoadhesive beads (F-O).
Mentions: In alloxan-induced diabetic rats, the comparative in vivo blood glucose level and the mean percentage reduction in blood glucose level after oral administration of pure glibenclamide and optimized glibenclamide-loaded IHM-alginate mucoadhesive beads (F-O) are presented in Figures 15 and 16, respectively. In case of the group treated with pure glibenclamide (Group A), a rapid reduction in blood glucose level was observed within 2-3 hours of administration, and after that, the blood glucose level recovered rapidly towards the normal level. In case of the group (Group B) treated with optimized glibenclamide-loaded IHM-alginate mucoadhesive beads, the reduction in blood glucose level was found slower than that of the group treated with pure glibenclamide (Group A) up to 3 hours. Significant differences (P < 0.05) were found between the blood glucose levels after administration of pure glibenclamide and optimized glibenclamide-loaded IHM-alginate mucoadhesive beads (F-O) at each time point measured. However, the reductions in glucose level were increased gradually with the increment of time in case of Group B (treated with optimized glibenclamide-loaded IHM-alginate mucoadhesive beads) and were sustained over 10 hours. A 25% reduction in glucose level is considered a significant hypoglycemic effect [29]. Therefore, the significant hypoglycemic effect by the optimized glibenclamide-loaded IHM-alginate mucoadhesive beads (F-O) was observed over 10 hours.

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.