Efavirenz-loaded intranasal microemulsion for crossing blood-CNS interfaces in neuronal-AIDS: pharmacokinetic and in vivo safety evaluation

Abstract Purpose: Development of delivery tool for the existing antiretroviral drugs against the neuronal-AIDS in itself is a big challenge because of blood-brain-barrier (BBB). Aim of present research is to formulate efavirenz (EFV) based mucoadhesive microemulsion (EMME) and investigates its efficiency through intranasal delivery. Methods: The EFV microemulsion (EME) was formulated by aqueous titration method. The formulation was screened for globule size, zeta potential and encapsulation efficiency. Bio-distribution of EFV was performed by gamma scintigraphy. Safety of optimized formulation was demonstrated using biochemical, hematological and histopathological data. Results: Experimental data demonstrate that optimized formulation showed significant size (19.04 nm), zeta potential (−32.2 mV) and entrapment efficiency (98.39%). The results of Cmax value suggested that intranasal (i.n.) 99mTc-EMME is able to improve the brain uptake of EFV around 2 folds more than i.n. 99mTC-EME and intravenous (i.v.) 99mTC-EME administrations. The drug targeting index (DTI= 10), drug targeting efficiency (DTE = 1000%) and direct transport percentage (DTP = 89%) were found highly significant for EMME (i.n.) than EME (i.n.). In vivo safety evaluation studies on experimental animals for biochemical, hematological and histopathological parameters remain unchanged. Conclusions: Hence, the intranasal delivery of EMME can be safe and effective tool in the treatment of neuronal-AIDS.

• Publication year

  2020

• Venue

  Pharmaceutical development and technology (Print)

• Publication date

  2020-01-02

• Fields of study

  Medicine

• Identifiers
  DOI 10.1080/10837450.2019.1659818PMID 31441694
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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