pH-sensitive chitosan nanoparticles loaded with dolutegravir as milk and food admixture for paediatric anti-HIV therapy

K Priya Dharshini; Hao Fang; D Ramya Devi; Jin-Xuan Yang; Rong-Hua Luo; Yong-Tang Zheng; Marek Brzeziński; B N Vedha Hari

doi:10.1016/j.carbpol.2020.117440

pH-sensitive chitosan nanoparticles loaded with dolutegravir as milk and food admixture for paediatric anti-HIV therapy

Carbohydr Polym. 2021 Mar 15:256:117440. doi: 10.1016/j.carbpol.2020.117440. Epub 2020 Nov 23.

Authors

K Priya Dharshini¹, Hao Fang², D Ramya Devi¹, Jin-Xuan Yang², Rong-Hua Luo³, Yong-Tang Zheng⁴, Marek Brzeziński⁵, B N Vedha Hari⁶

Affiliations

¹ Pharmaceutical Technology Laboratory, ASK-II, Lab No: 214, SASTRA Deemed-to-be-University, Thanjavur 613401, Tamil Nadu, India.
² Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China; College of Traditional Chinese Medicine, Yunnan University of Chinese Medicine, Kunming 650500, China.
³ Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China.
⁴ Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China. Electronic address: zhengyt@mail.kiz.ac.cn.
⁵ Centre of Molecular and Macromolecular Studies in Łódź, Polish Academy of Sciences, Sienkiewicza 112, 90-363 Lodz, Poland.
⁶ Pharmaceutical Technology Laboratory, ASK-II, Lab No: 214, SASTRA Deemed-to-be-University, Thanjavur 613401, Tamil Nadu, India. Electronic address: vedhahari@scbt.sastra.edu.

PMID: 33483020
DOI: 10.1016/j.carbpol.2020.117440

Abstract

The present study aims to develop Chitosan-based polymeric nanoparticles of anti-HIV drug Dolutegravir, to aid appropriate dose adjustment and ease of oral administration as milk and food admixture for children. The isolated Chitosan from the crab shell species Portunus Sanguinolentus has been characterized for their physicochemical properties. Nanoparticles were developed with varying ratio of drug: Chitosan and assessed for particle size (140-548 nm), zeta potential (+26.1 mV) with a maximum of 75 % drug content. Nanoparticles exhibited improved stability and drug release in the 0.1 N HCl medium compared to pure drug. The MTT assay and the Syncytia inhibition assay in C8166 (T-lymphatic cell line) infected with HIV_IIIB viral strain, which showed better therapeutic efficiency and lesser cytotoxicity compared to the pure drug. In consonance with the data obtained, the use of chitosan from a novel source for drug delivery carrier has opened exceptional prospects for delivering drugs efficiently to paediatrics.

Keywords: Biopolymer; Chitosan; Dolutegravir; Nanoparticle; Portunus sanguinolentus; Spray drying.

MeSH terms

Administration, Oral
Animal Shells
Animals
Anti-HIV Agents / pharmacology*
Biopolymers / chemistry
Cell Line
Child
Chitosan / chemistry*
Crustacea
Drug Carriers / chemistry*
Drug Liberation
Food
HIV Infections / drug therapy*
Heterocyclic Compounds, 3-Ring / administration & dosage*
Humans
Hydrogen-Ion Concentration
Kinetics
Magnetic Resonance Spectroscopy
Milk / chemistry*
Nanoparticles / chemistry*
Oxazines / administration & dosage*
Particle Size
Piperazines / administration & dosage*
Pyridones / administration & dosage*
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
Spray Drying
Temperature

Substances

Anti-HIV Agents
Biopolymers
Drug Carriers
Heterocyclic Compounds, 3-Ring
Oxazines
Piperazines
Pyridones
Chitosan
dolutegravir