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

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Preparation and Characterization of SDF-1α-Chitosan-Dextran Sulfate Nanoparticles
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Preparation and Characterization of SDF-1α-Chitosan-Dextran Sulfate Nanoparticles

Published on: January 22, 2015

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K Priya Dharshini1, Hao Fang2, D Ramya Devi1

  • 1Pharmaceutical Technology Laboratory, ASK-II, Lab No: 214, SASTRA Deemed-to-be-University, Thanjavur 613401, Tamil Nadu, India.

Carbohydrate Polymers
|January 23, 2021
PubMed

Insights

This study developed chitosan nanoparticles for the anti-HIV drug Dolutegravir, improving stability and delivery for children. These nanoparticles offer better therapeutic efficiency and lower toxicity than the pure drug.

Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Biotechnology

Background:

  • Pediatric HIV treatment requires optimized drug delivery systems for accurate dosing and palatability.
  • Chitosan, a biopolymer derived from crustacean shells, presents potential as a safe and effective drug carrier.
  • Dolutegravir is a key antiretroviral medication for managing HIV infections.

Purpose of the Study:

  • To formulate and characterize chitosan-based nanoparticles encapsulating Dolutegravir for pediatric oral administration.
  • To evaluate the physicochemical properties, stability, and drug release profile of the developed nanoparticles.
  • To assess the in vitro therapeutic efficacy and cytotoxicity of Dolutegravir-loaded chitosan nanoparticles.

Main Methods:

  • Chitosan was isolated from Portunus Sanguinolentus crab shells and characterized.
  • Polymeric nanoparticles were prepared using varying drug:chitosan ratios.
  • Particle size, zeta potential, and drug content were analyzed.
  • In vitro drug release studies were conducted in 0.1 N HCl.
  • Cytotoxicity was assessed using MTT assay, and antiviral activity was evaluated via Syncytia inhibition assay.

Main Results:

  • Chitosan nanoparticles exhibited particle sizes ranging from 140-548 nm with a positive zeta potential of +26.1 mV.
  • Maximum drug encapsulation efficiency reached 75%.
  • Nanoparticles demonstrated enhanced stability and improved drug release in acidic conditions compared to free Dolutegravir.
  • In vitro assays indicated superior therapeutic efficiency and reduced cytotoxicity for the nanoparticle formulation.

Conclusions:

  • Chitosan derived from Portunus Sanguinolentus is a viable material for developing effective Dolutegravir nanoparticles.
  • The developed nanoparticles offer a promising approach for improved oral drug delivery of Dolutegravir in pediatric patients.
  • This novel drug delivery system enhances therapeutic outcomes while minimizing adverse effects in children.

Keywords:
BiopolymerChitosanDolutegravirNanoparticlePortunus sanguinolentusSpray drying

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