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Fabrication of acyclovir-loaded flexible membrane vesicles (FMVs): evidence of preclinical efficacy of antiviral activity in murine model of cutaneous HSV-1 infection

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Abstract

The present investigation focuses on the development and evaluation of acyclovir-loaded flexible membrane vesicles (ACY-FMVs) and evaluates their targeting potential to localize the drug into skin layers. The drug-loaded FMVs were prepared by thin-film hydration method and characterized for various attributes including micromeritics, entrapment efficiency, vesicle shape, size, and degree of deformability. The values of particle size and zeta potential of the developed carrier system were found to be 453.7 nm and − 11.62 mV, respectively. The system was further incorporated into a hydrogel and evaluated for skin permeability and retention characteristics in comparison to marketed formulation. The developed formulation demonstrated enhanced retention of drug deep inside the skin layers which can probably decrease the frequency of application of the drug, thereby reducing its adverse effects. Skin irritancy studies performed on Laca mice skin proved the safety and non-irritant nature of ACY-FMVs. The pharmacodynamic studies on murine model for HSV-1 infection demonstrated immense potential and safety of topically applied ACY-FMVs. However, more intensive studies need to be pursued to explore and exploit the potential of lipid-based systems in anti-viral therapeutics. These preclinical findings provide a hope for corroborating the efficacy in clinical situations.

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Acknowledgements

Authors are thankful to M/s Ipca Laboratories Ltd., Mumbai, for generously providing the gift samples of acyclovir where as to M/s Phospholipid GmbH, Nattermannallee, Germany, for the ex-gratis supply of Phospholipids.

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Author notes

  1. Gajanand Sharma and Kanika Thakur contributed equally to this work

Authors and Affiliations

  1. University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Study, Panjab University, Chandigarh, 160014, India

    Gajanand Sharma, Kanika Thakur, Arvind Setia, Basant Amarji & Om Prakash Katare

  2. Department of Virology, Postgraduate Institute of Medical Education and Research, Chandigarh, 160012, India

    Mini P. Singh

  3. Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Dist. Ajmer, Kishangarh, Rajasthan, 305 817, India

    Kaisar Raza

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  1. Gajanand Sharma
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Correspondence to Kaisar Raza or Om Prakash Katare.

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Sharma, G., Thakur, K., Setia, A. et al. Fabrication of acyclovir-loaded flexible membrane vesicles (FMVs): evidence of preclinical efficacy of antiviral activity in murine model of cutaneous HSV-1 infection. Drug Deliv. and Transl. Res. 7, 683–694 (2017). https://doi.org/10.1007/s13346-017-0417-0

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