Design and Characterization of Anticancer Drug-Loaded Microspheres for Controlled Release
Mangesh P. Patil *
Parul Institute of Pharmacy, Parul University, Vadodra, Gujrat, India.
Chandrabhan B. Patil
Parul Institute of Pharmacy, Parul University, Vadodra, Gujrat, India.
Sumesh D. Patil
Parul Institute of Pharmacy, Parul University, Vadodra, Gujrat, India.
Purva M. Paprikar
Parul Institute of Pharmacy, Parul University, Vadodra, Gujrat, India.
Digvijay G. Patil
Parul Institute of Pharmacy, Parul University, Vadodra, Gujrat, India.
*Author to whom correspondence should be addressed.
Abstract
Microspheres refer to microparticles composed of a homogeneous mixture of active compounds and raw materials. Microsphere is a synonym of microparticle. Rectal drug delivery is an effective substitute for the oral and parenteral route of administration in partial avoidance of first-pass metabolism and protein peptide drug delivery. The rectum offers a relatively constant environment for drug delivery, provided the drug is presented in a well-absorbable form. The purpose of the present investigation was to prepare flutamide-loaded microspheres for a rectal drug delivery system with the aim of improving solubility, avoiding first-pass metabolism and enhancing residence time. Flutamide (FLT) was a gift sample from Cipla Pvt. Ltd. (Bangalore, India). Mucilage is extracted from Ocimum basilicum seeds (basil seed) in the laboratory, PEG4000, and Methanol. Flutamide is an anticancer drug that exhibits poor water solubility, poor dissolution and poor wetting. Flutamide encapsulated Mucoadhesive microsphere prepared by a simple one-step spray drying method using mucilage extracted from seeds of Ocimum basilicum as a natural polymer. The mucoadhesive microspheres were evaluated by different parameters such as percentage production yield, encapsulation efficiency study, particle size analysis, Differential Scanning Calorimeter (DSC), scanning electron microscopy (SEM), X-ray diffraction analysis (XRD), ex vivo mucoadhesive test, and in vitro drug release stability study. The microspheres were spherical with a size of 2.53µm. The encapsulation efficiency was observed from 57.44% to 69.67%, while the percentage of mucoadhesion was observed from 70.68% to 89.01%. The microsphere releases around 88.28 % of the drug in 7 hours. The DSC and XRD studies show that FLT was molecularly dispersed. It was concluded that Ocimum basilicum mucilage microsphere-based suppository could be used to deliver FLT to rectal drug administration for improving solubility, bioavailability, and avoiding first-pass metabolism.
Keywords: Mucoadhesive microsphere, Ocimum basilicum, flutamide, rectal delivery