臨床薬理学および生物薬剤学

抽象的な

Formulation and evaluation of drug phospholipid complex based self-Nano emulsifying drug delivery system (dpc-snedds) of bcs class iii drug: lisinopril

Md Shahnawaz Alam* ¸ Dr. Anoop Kumar¸ Pankaj pal

Poor bioavailability of a drug can be regarded as a consequence from two predominant factors if impaired permeation of drug across enterocytes and its poor aqueous solubility.This article intended to focus Drug Phospholipid Complexation (DPC) and its incorporation into SNEDDS as a dual delivery platform to improve drug bioavailability. Phospholipid complexation of drugs could bring out modulation in the intestinal permeability through inhibition of enzymatic activity via membrane perturbation of SNEDDS components, inhibition of membrane bound p-glycoprotein and efflux transporters. DPC components may allow switching over to lymphatic transport through chylomicron formation or enhancing the uptake of phospholipid vesicles through cellular internalization. It also addresses the challenges in the designing of DPC for highly soluble as well as poorly water-soluble drugs, methods of preparation and characterization. Various strategies to incorporate DPC into SNEDDS based systems and how it facilitates the drug characteristics through nanonization or micellization drug molecules are described. The organoleptic property of Lisinopril was determined by molecular weight, structure, melting point, FTIR and DSC. In the development of LPC- SNEDDS, Soy lecithin, Tween-80 and Polyethylene Glycol (PEG) 600 was selected based on the solubility and miscibility study. LPC-SNEDDS was prepared by simple mixing method and characterized. Optimized liquid LPC-SNEDDS formulation showed 232 nm droplet size, 0.438 PDI, -1.11 mV Zeta potential and 0.664 mS/cm electro conductivity. The Ex-vivo permeability of the optimized LPC-SNEDDS formulation showed 100 % drug release within 1hours and the Lisinopril suspension showed 54.9 % in 1 hours. The results obtained from studies in Wistar rats revealed distinct augmentation in permeability and absorption potential of the optimized formulations.