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

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 form...

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Main Authors: Mahmood, Syed, Kong, Chak Kiong, Chun, Shern Tham, Tan, Choo Chien, Ayah Rebhi, Hilles, Venugopal, Jayarama Reddy
Format: Article
Language:English
Published: Springer Science and Business Media Deutschland GmbH 2020
Subjects:
Q Science (General)
QL Zoology
Online Access:http://umpir.ump.edu.my/id/eprint/30858/1/AAPS%20PharmSciTech%202020%2021%20285.pdf
http://umpir.ump.edu.my/id/eprint/30858/
https://link.springer.com/content/pdf/10.1208/s12249-020-01810-0.pdf
https://doi.org/10.1208/s12249-020-01810-0
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spelling my.ump.umpir.308582021-09-23T04:51:00Z http://umpir.ump.edu.my/id/eprint/30858/ PEGylated lipid polymeric nanoparticle–encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation Mahmood, Syed Kong, Chak Kiong Chun, Shern Tham Tan, Choo Chien Ayah Rebhi, Hilles Venugopal, Jayarama Reddy Q Science (General) QL Zoology 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. Springer Science and Business Media Deutschland GmbH 2020-10-14 Article PeerReviewed pdf en http://umpir.ump.edu.my/id/eprint/30858/1/AAPS%20PharmSciTech%202020%2021%20285.pdf 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 https://link.springer.com/content/pdf/10.1208/s12249-020-01810-0.pdf https://doi.org/10.1208/s12249-020-01810-0
institution Universiti Malaysia Pahang
building UMP Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Malaysia Pahang
content_source UMP Institutional Repository
url_provider http://umpir.ump.edu.my/
language English
topic Q Science (General)
QL Zoology
spellingShingle Q Science (General)
QL Zoology
Mahmood, Syed
Kong, Chak Kiong
Chun, Shern Tham
Tan, Choo Chien
Ayah Rebhi, Hilles
Venugopal, Jayarama Reddy
PEGylated lipid polymeric nanoparticle–encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation
description 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.
format Article
author Mahmood, Syed
Kong, Chak Kiong
Chun, Shern Tham
Tan, Choo Chien
Ayah Rebhi, Hilles
Venugopal, Jayarama Reddy
author_facet Mahmood, Syed
Kong, Chak Kiong
Chun, Shern Tham
Tan, Choo Chien
Ayah Rebhi, Hilles
Venugopal, Jayarama Reddy
author_sort Mahmood, Syed
title PEGylated lipid polymeric nanoparticle–encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation
title_short PEGylated lipid polymeric nanoparticle–encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation
title_full PEGylated lipid polymeric nanoparticle–encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation
title_fullStr PEGylated lipid polymeric nanoparticle–encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation
title_full_unstemmed PEGylated lipid polymeric nanoparticle–encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation
title_sort pegylated lipid polymeric nanoparticle–encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation
publisher Springer Science and Business Media Deutschland GmbH
publishDate 2020
url http://umpir.ump.edu.my/id/eprint/30858/1/AAPS%20PharmSciTech%202020%2021%20285.pdf
http://umpir.ump.edu.my/id/eprint/30858/
https://link.springer.com/content/pdf/10.1208/s12249-020-01810-0.pdf
https://doi.org/10.1208/s12249-020-01810-0
_version_ 1712285316565434368
score 13.211869

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