Formulation and Evaluation of a Mucoadhesive Thermoresponsive System Containing Brazilian Green Propolis for the Treatment of Lesions Caused by Herpes Simplex Type I

J Pharm Sci. 2016 Jan;105(1):113-21. doi: 10.1016/j.xphs.2015.11.016. Epub 2016 Jan 13.

Abstract

The aim of the present work was to develop a topical delivery system that contains Brazilian green propolis extract (PE-8) to increase efficiency and convenience when applied to herpetic lesions. The cytotoxicity and antiherpetic activity was determined in vitro and in vivo. The PE-8 was added to a system that contained poloxamer 407 and carbopol 934P. The in vitro characterization of the system included rheological studies, texture profile analysis, and mucoadhesion analysis. The PE-8 inhibited the virus during the phase of viral infection, induced virion damage, and exhibited an ability to protect cells from viral infection. The system had advantageous mucoadhesive properties, including a suitable gelation temperature of approximately 25°C for topical delivery, a desirable textural profile, and pseudoplastic behavior. The in vitro release study showed a rapid initial release of the PE-8 in the first 3 h, and the rate of drug release remained constant for up to 24 h. The system appeared to be macroscopically and microscopically innocuous to skin tissue. Therefore, the mucoadhesive thermoresponsive system that contained the PE-8 appears to be promising for increasing bioavailability and achieving prolonged release of the PE-8 when applied to skin lesions caused by herpes simplex virus type 1.

Keywords: Brazilian green propolis; herpes simplex type I; mucoadhesive; rheology; viscoelastic.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylates / chemistry
  • Adhesiveness
  • Animals
  • Antiviral Agents / administration & dosage*
  • Antiviral Agents / chemistry
  • Antiviral Agents / therapeutic use
  • Antiviral Agents / toxicity
  • Cell Survival / drug effects
  • Chlorocebus aethiops
  • Dose-Response Relationship, Drug
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Female
  • Herpes Simplex / drug therapy*
  • Herpes Simplex / metabolism
  • Herpesvirus 1, Human / drug effects*
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mouth Mucosa / drug effects
  • Mouth Mucosa / metabolism
  • Mouth Mucosa / virology
  • Poloxamer / chemistry
  • Propolis / administration & dosage*
  • Propolis / chemistry
  • Propolis / therapeutic use
  • Propolis / toxicity
  • Rheology
  • Skin / drug effects
  • Skin / metabolism
  • Skin / virology
  • Temperature
  • Vero Cells

Substances

  • Acrylates
  • Antiviral Agents
  • Drug Carriers
  • Poloxamer
  • Propolis
  • carbopol 934P