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العنوان
Efficacy and bioavailability of a nano-formulation of praziquantel compared toa market form in murine schistosomiasis /
الناشر
Amr Mostafa Mohamed Mostafa Radwan ,
المؤلف
Amr Mostafa Mohamed Mostafa Radwan
هيئة الاعداد
باحث / Amr Mostafa Mohamed Mostafa Radwan
مشرف / Samira Saleh Mostafa
مشرف / Muhammad Yusuf Alshorbagy
مشرف / Sanaa Sabet Botros
تاريخ النشر
2020
عدد الصفحات
149 P. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
الصيدلة ، علم السموم والصيدلانيات (المتنوعة)
تاريخ الإجازة
14/9/2020
مكان الإجازة
جامعة القاهرة - كلية الصيدلة - Pharmacology and Toxicology
الفهرس
Only 14 pages are availabe for public view

from 192

from 192

Abstract

Schistosomiasis is responsible for a considerable global disease burden. This work aimed to improve the therapeutic outcome of the only available antischistosomal drug worldwide, praziquantel (PZQ), by incorporating it into a novel carrier, 2solid lipid nanoparticles (SLNs)3, to enhance its solubility, bioavailability and efficacy. Asimple, cost-effective formulations of PZQ in solid lipid nanoparticles were tested in this work in experimental murine schistosomiasis with the aim of enhancing PZQ solubility, bioavailability and efficacy. PZQ in nanoformulation may overcome its known drawbacks (quick first pass metabolism in the liver) with its consequent reduced efficacy, specifically against the immature forms in the systemic circulation. SLNs has a superior advantage over common nanoformulations with respect to drug targeting, release, long-shelf stability, low toxicity, better bioavailability and compatibility with several routes of administration.Moreover, SLNs could resolve drawbacks, including undesirable taste, possible irritation and gastrointestinal adverse reactions with high safety margins and high biocompatibility over other conventional nanoformulations. Compared to market PZQ (M{u2010}PZQ), SLN{u2010}PZQ was more bioavailable, as denoted by higher serum concentrations in both normal and infected mice where elevated Ka, AUC0{u2013}24, Cmax, and t1/2e with a decrease in kel were demonstrated. In normal and S. mansoni{u2010}infected mice, SLN{u2010}PZQ was detectable in serum at 24 h, while M{u2010}PZQ completely vanished 8 h post{u2010}treatment. Additionally, enhanced absorption with extended residence time was recorded for SLN{u2010}PZQ