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IJPER · Lens · Acyclovir Loaded Solid Lipid Nanoparticulate Gel for Ocular Delivery: Optimization by using Factorial Design

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Article · Volume 55, Issue 1s (Supplement) · pp. S122-S134

Acyclovir Loaded Solid Lipid Nanoparticulate Gel for Ocular Delivery: Optimization by using Factorial Design

Subhabrota Majumdar1, Suryakanta Swain2,3, Muddana Eswara Bhanoji Rao1, Puja Chakraborty1, Sabya Sachi Das4

  1. 1Calcutta Institute of Pharmaceutical Technology and AHS, Banitabla, Uluberia, Howrah, West Bengal, INDIA.
  2. 2School of Health Sciences, Department of Pharmaceutical Sciences, The Assam Kaziranga University, Jorhat, Assam-785006, INDIA.
  3. 3Southern Institute of Medical Sciences, College of Pharmacy, Department of Pharmaceutics, SIMS Group of Institutions, Mangaldas Nagar, Vijayawada Road, Guntur, Andhra Pradesh, INDIA.
  4. 4Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, INDIA.

Abstract

Background: Acyclovir is a potent antiviral agent primarily used to treat viral infection in the eye, signified as Herpes Simplex Keratitis caused by Herpes Simplex Virus-1. But its applications are limited because of its poor oral bioavailability and permeability caused by significant first-pass metabolism.Objectives: The study is to design the formulation, optimization, in-vitro, ex-vivo and in-vivo characterization of solid lipid nanoparticulate gel (SLNG) of acyclovir and inspect their possibility in ocular applications.Methods: SLNG of acyclovir was prepared by hot homogenization technique and optimized by 23 factorial design and evaluated for in-vitro physicochemical characteristics and in-vivo pharmacokinetic study. Response surface methodology estimations and plots for optimization to obtain optimum values for response variables based on desirability criteria was performed using Design-Expert software.Results: The optimized formulation showed a particle size of 193.57±1.14 nm, zeta potential of 35±1.98 mv, drug entrapment efficiency of 82±1.59% and drug loading efficiency of 54.10±0.79%, indicating good physical stability. The transcorneal study showed a significant increase in drug permeation across the cornea as compared with the control. The drug release kinetics of the prepared formulations was best fitted to the first-order kinetic model. In-vivo pharmacokinetic studies revealed a significant enhancement in the drug level in the blood plasma of the optimized formulation as compared to the pure drug suspension.Conclusion: The acyclovir-loaded SLN gel was successfully developed, optimized, evaluated and exhibited enhanced drug permeation as well as systemic bioavailability through excised corneas. Thus, SLNG acts as a favorable approach for ocular applications of acyclovir.

Keywords: Acyclovir; Hot homogenization; Factorial design; Drug entrapment efficiency; Transcorneal study; Pharmacokinetic study

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