Formulation and Evaluation of Topical Linezolid Nanoemulsion for Open Incision Wound in Diabetic Animal Model

AAPS PharmSciTech. 2022 Apr 28;23(5):129. doi: 10.1208/s12249-022-02288-8.

Abstract

The present study aimed to investigate the role of topical nanoemulsion of linezolid in attenuating diabetic wound by delivering the drug to the target tissue. The nanoemulsions (NEs) were prepared by high-pressure homogenization and subjected to thermodynamic stability, pH, droplet size, viscosity, surface charge, polydispersity index (PDI), entrapment efficiency, drug content, and in vitro drug release. All formulations were thermodynamically stable. The pH was in the range of 5 to 6. The viscosities of LZD-0, LZD-1, LZD-2, and LZD-3 were recorded as 68.75 ± 2.23 mPas, 69.56 ± 2.11 mPas, 96.45 ± 3.39 mPas, and 45.5 ± 1.12 mPas respectively. LZD-1 exhibited droplet size of 376.5 nm ± 0.98, surface charge - 22.5mV, and PDI 0.387. Drug content and entrapment efficiency of LZD-1 were found to be 93 ± 3.31 % and 72 ± 1.67 %, respectively. LZD-1 released 80 ± 2.87% of drug. Due to significant (P < 0.05) in vitro results, LZD-1 formulation was selected for in vivo evaluation. Diabetes was induced in Sprague-Dawley rats using intraperitoneal streptozotocin injection at dose of 50 mg/kg. Open-incision wounds were inflicted among all diabetic rats at dorsal shaved area. Randomly, all rats were divided into positive control (blank formulation), negative control (no formulation), and test group (LZD-1). Wound healing occurred in order of test group > positive control > negative control. Skin histology and tensile strength also revealed significant results. The study concluded that topical nanoemulsion of linezolid may open new horizon in treating diabetic wounds.

Keywords: Nigella sativa; diabetic wound; linezolid; topical nanoemulsion.

MeSH terms

  • Animals
  • Diabetes Mellitus, Experimental* / drug therapy
  • Disease Models, Animal
  • Emulsions / chemistry
  • Linezolid
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Emulsions
  • Linezolid