Development and Evaluation of Nanosuspension Incorporated in situ gel of Brimonidine Tartarate for Ocular Drug Delivery

ABSTRACT

Objectives: The goal of the study was to develop, optimize and in vitro-ex vivo investigation of Brimonidine tartrate nanosuspension incorporated in situ gel formulation to differentiate with marketed (formulation) eye drops for the efficient treatment of glaucoma. Materials and Methods: Nanosuspensions were formulated by solvent evaporation method using probe sonication technique. The effect of the independent variables Tween 80 and Pluronic F68 concentration on Nanosuspension properties were investigated by performing 32 factorial design of experiment. Nanosuspensions were characterized by measuring particle diameter and zeta potential, surface morphology, drug entrapment efficiency and then nanosuspensions were incorporated in to in situ gel base for in vitro release and ex-vivo corneal permeability studies and were differentiated with marketed product. Results and Discussion:The most excellent nanosuspension formulation system selected via the Design Expert 12 software program was F7 which contains 0.5% of Tween 80 and 3 % of Pluronic F68. An optimized nanosuspension formulation F7 showed an average particle diameter of 157.4±0.95 nm with PDI of 0.379 and a zeta potential of -19.1 mV. It had an average entrapment efficiency of 85.95±1.40%. It also showed 98.36±0.58% of drug being released in vitro when incorporated in to in situ gel base over 24 hr. F7 showed significantly greater drug permeation in comparison to the marketed eye drop formulation in ex vivo transcorneal permeability studies and was able of retaining its stability for 90 days. Conclusion: The developed nanosuspension incorporated in situ gel base formulation could be utilized as potential delivery system for long time management of glaucoma with once daily dose.

KEYWORDS

• Brimonidine Tartrate
• Ocular bioavailability
• Nanosuspension
• In-situ gel
• Increased residence time

Showing references and in-text citations exactly as published.

• DOI10.5530/ijper.56.1.12Copy

RELATED ARTICLES

Matched on section and article type within this issue of IJPER.

• Article · VOLUME 56, ISSUE 1Development of Magnetic Nanoparticles and Encapsulation Methods – An OverviewVenkata Satya Madhulatha, E Susithra, Raghavendra Kumar Gunda · pp. 1–8Original ArticleSame type: Article
• Article · VOLUME 56, ISSUE 1Telepharmacy Knowledge, Perceptions, and Readiness among Future Malaysian Pharmacists Amid the COVID-19 PandemicMohamed Hassan Elnaem, Muhammad Eid Akkawi, Abdul Kareem Al-Shami, Ramadan Elkalmi · pp. 9–16Original ArticleSame type: Article
• Article · VOLUME 56, ISSUE 1Perspectives of Pharmacy University Students on Scientific Research in Comparison to Students from Other Health Science DisciplinesSyed Mohammed Basheeruddin Asdaq, Mohammed Kanan Alshammari, Bassam Mohammed Alanazi, Ahmed Naif Alshammari, Mishal Abdulrahman Alrumaih, Mohd. Imran, Abdulhakeem S Alamri, Majid Alhomrani, Walaa F. Alsanie, Nagaraja Sreeharsha · pp. 17–23Original ArticleSame type: Article
• Article · VOLUME 56, ISSUE 1New Approach of Dipterocarpus alatus Oil as a Permeation Enhancer in Ibuprofen GelSupawadee Daodee, Orawan Monthakantirat, Yaowared Chulikhit · pp. 24–31Original ArticleSame type: Article