Synthesis and Characterization of Valacyclovir HCl Hybrid Solid Lipid Nanoparticles by Using Natural Oils

Recent Pat Drug Deliv Formul. 2019;13(1):46-61. doi: 10.2174/1872211313666190304142129.

Abstract

Background: The Jojoba Simmondsia Chinensis oil is used as one of the main ingredients which has an antioxidant, moisturizing and stabilizing activity. Likewise, grape seed (Vitis vinifera) oil is also used in this preparation which also has some remarkable medicinal properties such as antioxidant, astringent and is also used as a moisturizer. The Valacyclovir Solid Lipid Nanoparticles (SLN) are prepared in combination.

Objective: The prime objective of the study was to prepare a nanodispersion with good stability indicating zeta potential. The formulations were prepared by varying concentrations of jojoba oil and grape seed oil which form the hybrid nanoparticles with the drug.

Methods: The high-pressure hot-homogenization technique was used to prepare the nanoparticles. The prepared nanoparticles were subjected to characterization analysis such as Mean particle size, Zaverage, and Zeta potential by using Dynamic Light Scattering (DLS) and Photon Correlation Spectroscopy (PCS). The best formulation was subjected to Transmission Electron Microscopy (TEM) technique for surface morphology and other characterizations. The crystalline pattern of the drug alone, drug-loaded nanoparticles and nanoparticles without the drug was studied by XRD. The drug excipients compatibility studies were performed by using Fourier-Transform Infrared Spectroscopy (FTIR) Differential Scanning Calorimetry and (DSC). The other factors such as in vitro drug release, and % drug entrapment efficiency were studied by using suitable methods.

Results: The results demonstrated that the particles are in nano range with good stability with appreciable Zeta potential (-48.2±mV). The selected formulations were analyzed for MPS which demonstrated the value of 306.7±183.4 and 416.5±289.3. The best formulation VNP5 demonstrated the Bellshaped curve and confirmed the uniform distribution.

Conclusion: Based on the patents, it was demonstrated that valacyclovir is widely used in the treatment and prophylaxis of viral infections in human, particularly infections caused by the herpes group of viruses. Valacyclovir is an effective drug for the treatment of cold sores.

Keywords: DSC; FTIR; SLN; TEM; XRD; valacyclovir; zeta potential..

MeSH terms

  • Animals
  • Antiviral Agents / administration & dosage
  • Antiviral Agents / chemical synthesis
  • Chemistry, Pharmaceutical / methods
  • Drug Delivery Systems / methods
  • Grape Seed Extract / administration & dosage
  • Grape Seed Extract / chemical synthesis
  • Lipids / administration & dosage
  • Lipids / chemical synthesis*
  • Nanoparticles / chemistry*
  • Patents as Topic*
  • Plant Oils / administration & dosage
  • Plant Oils / chemical synthesis*
  • Rats
  • Rats, Wistar
  • Skin Absorption / drug effects
  • Skin Absorption / physiology
  • Valacyclovir / administration & dosage
  • Valacyclovir / chemical synthesis*
  • X-Ray Diffraction / methods

Substances

  • Antiviral Agents
  • Grape Seed Extract
  • Lipids
  • Plant Oils
  • Valacyclovir