Electronic Theses and Dissertations

Date of Award

1-1-2023

Document Type

Dissertation

Degree Name

Ph.D. in Pharmaceutical Sciences

First Advisor

Soumyajit Majumdar

Second Advisor

Michael A. Repka

Third Advisor

Seongbong Jo

School

University of Mississippi

Relational Format

dissertation/thesis

Abstract

Ocular drug delivery faces many challenges due to the unique anatomy and physiology of the human eye. The development of ocular drug delivery systems is subjected to a gradual shift from an empirical to a rational base due to a better understanding of the ocular barriers that control drug disposition in the eyeball as well as new approaches in clinical testing. Most of the topically applied actives are lipophilic with low aqueous solubility, and the ocular delivery of these drugs is posing a challenging task. Lipid-based drug delivery systems are well reported to improve solubility and enhance both bioavailability and penetration of drugs into deep intraocular tissues. Therefore, lipid-based nanoformulations loaded with ciprofloxacin, moxifloxacin, and cannabidiol and its analog (cannabidiol-valine-hemisuccinate) were prepared and investigated with the intent to improve solubility, prolong drug residence on the ocular surface, and improve ocular drug permeation and penetration for improved ocular delivery of these drugs. Chapter 1 discusses eye anatomy and physiology, barriers to ocular drug delivery, commercial ocular dosage forms, and lipid-based nanocarriers for ocular drug delivery in brief. Chapter 2 reports the preparation of ciprofloxacin-loaded nanostructured lipid carriers incorporated into in situ gels to improve the management of bacterial endophthalmitis. The lead formulations were stable over three months and demonstrated extended-release profiles over a 24 h period. The transcorneal flux and permeability increased significantly from both formulations when compared to the commercial solution eyedrops. Chapter 3 discusses the design of topical moxifloxacin mucoadhesive nanoemulsion for the management of ocular bacterial infections. The lead formulations showed desired physicochemical properties and viscosity. Ex vivo transcorneal permeation studies exhibited significant improvement in drug permeation compared with solution eyedrops. Moreover, the lead formulations showed similar in vitro antibacterial activity as the commercial eyedrops. Chapter 4 discusses the formulation development and in vitro-ex vivo evaluation of cannabidiol and cannabidiol-valine-hemisuccinate lipid-based nanoformulations for ocular applications. The transcorneal permeation studies revealed improvement in permeability and flux for CBD and its analog from the lead formulations. In conclusion, the prepared formulations could serve as efficient delivery systems for improving the ocular delivery of the drugs under these investigations.

Available for download on Saturday, September 13, 2025

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