DEVELOPMENT, SCREENING AND OPTIMIZATION OF ROSUVASTATIN LOADED NANOSTRUCTURED LIPID CARRIERS FOR IMPROVED THERAPEUTIC EFFICACY

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

doi:10.22270/ujpr.v9i5.1212

El Sayed Gamal E. Shaheen Pharmaceutics Department, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt.
Walid Anwar 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.v9i5.1212

Keywords:

Glyceryl monostearate, nanostructured lipid carriers, optimization, rosuvastatin calcium

Abstract

Objective: The aim of the current study was to be screening of the formulation components, prepare ROS-NLCs by hot homogenization–ultrasonication technique and optimized by Full factorial design then formulations prepared were further characterized.

Methods: The screening experiments were carried out to select the most suitable solid lipids, liquid lipids, and surfactants. Moreover, physical compatibility between the solid lipids and liquid lipids, along with their proportions, was evaluated. Additionally, characterization and optimization of the developed formulations were outlined and identified. Primarily, the solubility of ROS-Ca in various solid lipids and liquid lipids is the key factor for choosing the optimal one.

Results: Stearic acid, Glyceryl Monostearate (GMS), and Compritol®888 ATO exhibited a higher ability to solubilize ROS-Ca, with solid lipid values per 10 mg of ROS-Ca (w/w) recorded as 750±3.56 mg, 1250±4.36 mg, and 1750±5.16 mg, respectively. In the systematic screening of different liquid lipids, Transcutol® HP (98.41 mg/ml), CapryolTM90 (78.64 mg/ml), and Labrafac MC60 (64.36 mg/ml) demonstrated a good affinity for the drug. The (Stearic acid-Transcutol® HP) mixture showed phase separation with oil droplet residue on filter paper, whereas the (GMS-Transcutol® HP) mixture showed no separation and left no oil droplet residue on filter paper. The optimized NLC formulations composed of glyceryl monostearate GMS (solid lipid) and Transcutol® HP (liquid lipid) as lipid phase, poloxamer 188 and Tween 80 (1:1 ratio) as surfactants.

Conclusions: Study concludes the ability of NLCs to improve the oral bioavailability of poorly water-soluble drugs by enhancing solubilization and dissolution rates in the gastrointestinal tract is well-recognized.