Preparation and evaluation of celecoxib-loaded microcapsules with self-microemulsifying core.
The purpose of this study was to prepare alginate microcapsules with a self-microemulsifying system (SMES) containing celecoxib in the core. An Inotech IE-50 R encapsulator equipped with a concentric nozzle was used to prepare the microcapsules. The encapsulated SMES was shown to increase celecoxib solubility over that of the pure drug more than 400-fold. Microcapsules prepared with a high SMES:celecoxib ratio exhibited distinct core vesicles containing liquid SMES. By modifying the SMES and including an additional chitosan coating, drug loading in the range from 12-40% could be achieved with the degree of encapsulation ranging from 60-82%. Alginate microcapsules loaded with SMES and celecoxib showed increased dissolution rate of celecoxib over that of alginate microcapsules loaded with celecoxib or of the celecoxib alone. Compared to the previous report, drug loading capacity was significantly improved, enabling the formulation of dosage forms which are of suitable size for peroral application.
Homar
Miha
M
Lek Pharmaceuticals d.d., Sandoz Development Center Slovenia, Ljubljana, Slovenia.
Dreu
Rok
R
Kerc
Janez
J
Gasperlin
Mirjana
M
D000464:Alginates / Q000737:chemistry*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage*; D002214:Capsules / Q000737:chemistry*; D000068579:Celecoxib; D004655:Emulsions / Q000737:chemistry; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D011720:Pyrazoles / Q000008:administration & dosage*; D012995:Solubility; D013449:Sulfonamides / Q000008:administration & dosage*
D000464:Alginates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D002214:Capsules; D004655:Emulsions; D006603:Hexuronic Acids; D011720:Pyrazoles; D013449:Sulfonamides; D020723:Glucuronic Acid; D000068579:Celecoxib