International Journal of Pharmaceutical Investigation, 2011, 1, 1, 10-16.
DOI: 10.4103/2230-973X.76722
Published: February 2011
Type: Invited Article
Authors:
Yatendra Kumar
Department of Pharmaceutics, Rajiv Academy for Pharmacy, NH#2, P.O. Chhattikara, Mathura-281 001, India.
Betty Philip
Department of Pharmaceutics, Rajiv Academy for Pharmacy, NH#2, P.O. Chhattikara, Mathura-281 001, India.
Kamla Pathak
Department of Pharmaceutics, Rajiv Academy for Pharmacy, NH#2, P.O. Chhattikara, Mathura-281 001, India.
ABSTRACT
Aim: The aim of the project was to develop cross-linked β-cyclodextrin (CL β-CD) microparticles for controlled delivery of a highly water-soluble drug. Materials and Methods: CL β-CD microparticles were prepared by emulsifi cation phase separation technique using epichlorohydrin as a cross-linking reagent. The developed microparticles were compared with β-CD for their pharmacotechnical properties. A highly water-soluble model drug, pravastatin sodium (PS) was loaded within these hydrophobic microparticles by active drug loading method using nonionic surfactant Tween 80 as the loading facilitator. Results: Maximal drug fi xation (216.8 mg/g beads) was observed in pH 4 at 20°C. In vitro release studies of PS-loaded CL β-CD microparticles in simulated gastric fl uid and simulated intestinal fl uid resulted in modifi ed dissolution profi les. Modeling of release profi les confi rmed controlled release (r2 = 0.9910) of PS from the cross-linked system. Conclusion: Controlled release CL β-CD microparticles PS that have the potential to enhance its therapeutic properties by offering the advantage of less frequent dosing and decreased fl uctuations in the blood levels during the dosing interval were successfully developed.
Keywords: Cross-linked β-cyclodextrin, Pravastatin sodium, Drug loading, Controlled release.