PEGylated Lipid Polymeric Nanoparticle–Encapsulated Acyclovir for In Vitro Controlled Release and Ex Vivo Gut Sac Permeation

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.

Development and Optimization of Hybrid Polymeric Nanoparticles of Apigenin: Physicochemical Characterization, Antioxidant Activity and Cytotoxicity Evaluation

“…The ON2 showed the APC of 32.87 × 10 −4 cm/s which is 3.8-fold higher than the pure AN (12.94 × 10 −4 cm/s). The low permeation of pure AN is due to the thickness and small porosity of the intestine and the high wide clearance of the intestinal P-gp efflux [ 47 ]. The significantly high permeation of the ON2 is due to the nano size and high surface area of formulation over the intestinal area [ 48 ].…”

Formulation of Piperine Nanoparticles: In Vitro Breast Cancer Cell Line and In Vivo Evaluation

“…An increment in the PL-90G concentration from 75 mg to 125 mg significantly increases the viscosity of organic solution during the preparation that significantly increases the heterogeneity among the PPN-LPHNPs, which produce LPHNPs with high PDI [ 39 ]. Furthermore, an increment in the CS concentration from 40 mg to 80 mg supports the formation of coarse dispersion during the preparation due to lack of energy to combat the viscous forces and produce PPN-LPHNPs with high PDI [ 40 ]. Moreover, the PDI of PPN-LPHNPs significantly reduces on increasing the amount of P-188 (coded as “C”).…”

Ibuprofen-Loaded Chitosan–Lipid Nanoconjugate Hydrogel with Gum Arabic: Green Synthesis, Characterisation, In Vitro Kinetics Mechanistic Release Study and PGE2 Production Test

“…Its temperature was maintained at 32 ± 0.5 °C to maintain skin surface temperature and mimic in vivo conditions, using a re-circulating water bath. The solution in the receptor chambers was stirred continuously at 100 rpm [ 55 , 56 ]. A quantity of 50 mg of the S3 and S6 formulations tested was placed in the donor compartment and spread evenly on the cellulose membrane.…”