CHITOSAN COATED ROSUVASTATIN NANOSTRUCTURED LIPID CARRIERS: FORMULATION, IN VITRO CHARACTERIZATION AND STORAGE ASSESSMENTS

Walid Anwar; El Sayed Gamal E. Shaheen; Sherif K. Abu-Elyazid; Mohsen I. Afouna

doi:10.22270/ujpr.v10i3.1363

Walid Anwar Pharmaceutics Department, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt.
El Sayed Gamal E. Shaheen Pharmaceutics Department, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt.
Sherif K. Abu-Elyazid Pharmaceutics Department, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt.
Mohsen I. Afouna Pharmaceutics Department, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt.

10.22270/ujpr.v10i3.1363

Keywords:

Glyceryl monostearate, hyperlipidemia, nanostructured lipid carriers, Rosuvastatin calcium

Abstract

Background and Objective: Rosuvastatin calcium (ROS-Ca) is a synthetic, highly potent third-generation HMG-CoA reductase inhibitor with significant hypocholesterolemic effects. The objective of this study was to develop and characterize nanostructured lipid carriers (NLCs) as a delivery system for the poorly water-soluble drug rosuvastatin calcium (ROS-Ca), with the aim of enhancing its dissolution rate and improving oral bioavailability.

Methods: ROS-NLCs is prepared by hot homogenization–ultrasonication technique then the prepared formulations were further characterized. Finally compare their characteristics to the corresponding a positively charged chitosan coated to develop new CH-ROS-NLCs. In this study, glyceryl monostearate (GMS) was selected as solid lipids and Transcutol® HP as a liquid lipid, to develop ROS-NLC (nanostructured lipid carrier).

Results: The physicochemical properties were achieved. The prepared ROS-NLC formulation was showed in nanometric size (121.6±6.2 nm) with encapsulation efficiency (63±0.2%). Furthermore, ROS-NLC and CH-ROS-NLC appeared almost spherical nanoparticles in morphology under transmission electron microscope (TEM). DSC, XRD and FT-IR analysis showed that ROS was miscible, compatible, and incorporated into NLCs in amorphous form not in native crystalline state.

Conclusion: The previously results showed that ROS-Ca was successfully encapsulated into nanostructured lipid carriers (NLCs) which coated with chitosan CH-ROS-NLC to overcome the above-mentioned defects and, it was ensured that nanostructured lipid carriers have high beneficial effect for enhancing and improving the oral bioavailability of poorly water-soluble drugs such as Rosuvastatin.