تاريخ مجلس الدراسات العليا

2023-01-08

اسم الطالب

تمارا احمد جميل العتيبي

ملخص الرسالة

Pilocarpine hydrochloride is a non-selective muscarinic receptor agonist that is prescribed for the treatment of glaucoma. The use of pilocarpine conventional eye drops is associated with several side effects, especially for elderly people. Such adverse effects can lead to low patient compliance, and hence poor clinical outcomes. Therefore, the aim of this project was to develop, optimize and characterize a pilocarpine ocular insert using niosomes are a delivery vehicle for the drug. Various polymers were investigated for the development of blank films, namely hydroxy propyl methyl cellulose (HPMC), polyvinyl alcohol (PVA) and a combination of both materials. The produced blank films were characterized based on evaluation criteria, weight uniformity and disintegration time. Niosomes of pilocarpine were prepared by thin film hydration method using span 60 and cholesterol with a ratio of 2:1, respectively. These niosomes were characterized based on structural microscopy, Fourier Transform Infrared Spectroscopy (FTIR) analysis and entrapment efficiency. The loaded insert containing 1 or 2 mg pilocarpine, were further evaluated for weight uniformity, moisture and content uniformity, thickness, and in vitro release pattern. X-ray diffraction (XRD) and Differential scanning calorimetric (DSC) analysis for pilocarpine, niosomes and films were further carried out. Results indicated that blank films made of the two polymers were better than single polymer-based films, based on the evaluation criteria; especially batch number F30 and F33 (have high evaluation scores). The formed niosomes demonstrated good entrapment efficiency 49.7% ±7.0, with an average particle size of 325.7 ± 3.5 nm. The FTIR analysis showed no interaction between the compositions of niosomes. The resulted drug loaded inserts provided uniformity in the content (89-96%) and with 34.8% moisture content and an average pH=7. The release profile of drug loaded inserts demonstrated an initial burst release within 2 hours and continuous sustained release for the next 24 hours ranging from 50-90% according to the formulation type and load. Overall, this project was able to successfully develop, optimize and characterize inserts containing slow-release pilocarpine encapsulated in niosomes for the potential ocular use. Further work will be commenced in the future to evaluate the stability of the produced inserts.