Polylactic acid and polyethylene glycol diblock copolymers of two different ratios, 90:10 and 70:30, were synthesized by melt polymerization. Antitubercular drugs, including rifampin, isoniazid, and pyrazinamide nanocarriers of PLEG 90:10 and 70:30, were synthesized by single emulsion evaporation and analyzed by FTIR, 1H, 13C NMR, and electron microscope. The hydrophobicity of PLEG copolymer decreased with the increasing concentration of polyethylene glycol, 78.1 ± 0.97 for 10 mol% PEG and 62.1 ± 0.89 for 30 mol% PEG. Drug-loaded nanocarriers appeared spherical with a diameter of 215 nm ± 21.2. High drug release for all the antitubercular drugs was observed with PLEG 70:30 both in vitro and in vivo. Maximum bioavailability was observed with intravenous administration for about 48 h. Our results prove that PLEG based nanocarriers are a potential drug carrier system for tuberculosis owing to the enhanced drug stability, sustained drug release, and increased bioavailability.

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Evaluation of Antitubercular Drug Release Kinetics from Polylactic Acid - Polyethylene Glycol Diblock Nano- Carriers

  • Malathi Sampath,
  • Nandakumar Venkatesan,
  • Saravanan Selvaraj,
  • Vinodhini Sridharan,
  • Ezhilarasu Tamilarasu,
  • Balasubramanian Sengottuvelan

摘要

Polylactic acid and polyethylene glycol diblock copolymers of two different ratios, 90:10 and 70:30, were synthesized by melt polymerization. Antitubercular drugs, including rifampin, isoniazid, and pyrazinamide nanocarriers of PLEG 90:10 and 70:30, were synthesized by single emulsion evaporation and analyzed by FTIR, 1H, 13C NMR, and electron microscope. The hydrophobicity of PLEG copolymer decreased with the increasing concentration of polyethylene glycol, 78.1 ± 0.97 for 10 mol% PEG and 62.1 ± 0.89 for 30 mol% PEG. Drug-loaded nanocarriers appeared spherical with a diameter of 215 nm ± 21.2. High drug release for all the antitubercular drugs was observed with PLEG 70:30 both in vitro and in vivo. Maximum bioavailability was observed with intravenous administration for about 48 h. Our results prove that PLEG based nanocarriers are a potential drug carrier system for tuberculosis owing to the enhanced drug stability, sustained drug release, and increased bioavailability.