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PEGylated lipid polymeric nanoparticle–encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation

Mahmood, Syed and Kong, Chak Kiong and Chun, Shern Tham and Tan, Choo Chien and Ayah Rebhi, Hilles and Venugopal, Jayarama Reddy (2020) PEGylated lipid polymeric nanoparticle–encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation. AAPS PharmSciTech, 21 (7). pp. 1-15. ISSN 1530-9932

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Abstract

Currently, pharmaceutical research is directed wide range for developing new drugs for oral administration to target disease. Acyclovir formulation is having common issues of short half-life and poor permeability, causing messy treatment which results in patient incompliance. The present study formulates a lipid polymeric hybrid nanoparticles for antiviral acyclovir (ACV) agent with Phospholipon® 90G (lecithin), chitosan, and polyethylene glycol (PEG) to improve controlled release of the drugs. The study focused on the encapsulation of the ACV in lipid polymeric particle and their sustained delivery. The formulation developed for the self-assembly of chitosan and lecithin to form a shell encapsulating acyclovir, followed by PEGylation. Optimisation was performed via Box-Behnken Design (BBD), forming nanoparticles with size of 187.7 ± 3.75 nm, 83.81 ± 1.93% drug-entrapped efficiency (EE), and + 37.7 ± 1.16 mV zeta potential. Scanning electron microscopy and transmission electron microscopy images displayed spherical nanoparticles formation. Encapsulation of ACV and complexity with other physical parameters are confirmed through analysis using Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. Nanoparticle produced was capable of achieving 24-h sustained release in vitro on gastric and intestinal environments. Ex vivo study proved the improvement of acyclovir’s apparent permeability from 2 × 10−6 to 6.46 × 10−6 cm s−1. Acyclovir new formulation was achieved to be stable up to 60 days for controlled release of the drugs.

Item Type: Article
Additional Information: Indexed by Scopus
Uncontrolled Keywords: Acyclovir; Hybrid nanoparticles (LPHNs); Box-Behnken design; In vitro; Ex vivo permeation
Subjects: Q Science > Q Science (General)
Q Science > QL Zoology
Faculty/Division: Centre of Excellence: Centre of Excellence for Advanced Research in Fluid Flow
Faculty of Industrial Sciences And Technology
Faculty of Chemical and Process Engineering Technology
Depositing User: Prof. Dr. Jayarama Reddy Venugopal
Date Deposited: 23 Sep 2021 04:51
Last Modified: 23 Sep 2021 04:51
URI: http://umpir.ump.edu.my/id/eprint/30858
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