Tarek A Ahmed1, Khalid M El-Say2. 1. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, P.O. Box 80200, 21589 Jeddah, Saudi Arabia; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt. Electronic address: dr_tarek_nour@yahoo.com. 2. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, P.O. Box 80200, 21589 Jeddah, Saudi Arabia; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
Abstract
AIMS: First; to develop rabeprazole (RP)-alginate core coated chitosan nanoparticles (NP) utilizing water in oil (W/O) nanoemulsion technique. Second; formulation of transdermal patches loaded RP-NP that avoid drug peroral acid sensitivity and first pass effect. MAIN METHODS: The influence of six factors on RP-NP formulation was investigated using Plackett-Burman (PB) design. The studied factors were considered for their effect on particle size (Y1) and loading efficiency (Y2). Formulation optimum desirability was identified; a proposed formulation was prepared and characterized. In vitro permeation of the prepared NP compared with RP was studied. Transdermal patches loaded drug or RP-NP were prepared and characterized. Patches ex vivo permeation through rat skin was studied, and kinetic analysis and permeation mechanism were investigated. KEY FINDING: Chitosan, oil phase and surfactant to oil ratios had significant effects on Y1, while Y2 was significantly affected by the same variables affecting Y1 and span80-tween80 ratio. Scanning electron microscope imaging illustrated sphericity of the NP. The optimized RP-NP exhibited sustained release pattern. The prepared patches showed a minimal patch to patch variable. Patches loaded RP-NP exhibited substantial skin permeability and controlled drug release, and were in favor of Fickian diffusion. SIGNIFICANCE: Transdermal patches loaded RP-NP is effective drug delivery and alternative to drug peroral route.
AIMS: First; to develop rabeprazole (RP)-alginate core coated chitosan nanoparticles (NP) utilizing water in oil (W/O) nanoemulsion technique. Second; formulation of transdermal patches loaded RP-NP that avoid drug peroral acid sensitivity and first pass effect. MAIN METHODS: The influence of six factors on RP-NP formulation was investigated using Plackett-Burman (PB) design. The studied factors were considered for their effect on particle size (Y1) and loading efficiency (Y2). Formulation optimum desirability was identified; a proposed formulation was prepared and characterized. In vitro permeation of the prepared NP compared with RP was studied. Transdermal patches loaded drug or RP-NP were prepared and characterized. Patches ex vivo permeation through rat skin was studied, and kinetic analysis and permeation mechanism were investigated. KEY FINDING: Chitosan, oil phase and surfactant to oil ratios had significant effects on Y1, while Y2 was significantly affected by the same variables affecting Y1 and span80-tween80 ratio. Scanning electron microscope imaging illustrated sphericity of the NP. The optimized RP-NP exhibited sustained release pattern. The prepared patches showed a minimal patch to patch variable. Patches loaded RP-NP exhibited substantial skin permeability and controlled drug release, and were in favor of Fickian diffusion. SIGNIFICANCE: Transdermal patches loaded RP-NP is effective drug delivery and alternative to drug peroral route.
Authors: Mohammad A S Abourehab; Rahul R Rajendran; Anshul Singh; Sheersha Pramanik; Prachi Shrivastav; Mohammad Javed Ansari; Ravi Manne; Larissa Souza Amaral; A Deepak Journal: Int J Mol Sci Date: 2022-08-12 Impact factor: 6.208