دورية أكاديمية
أعرض في EDS

Stabilized oral nanostructured lipid carriers of Adefovir Dipivoxil as a potential liver targeting: Estimation of liver function panel and uptake following intravenous injection of radioiodinated indicator.

التفاصيل البيبلوغرافية
العنوان: Stabilized oral nanostructured lipid carriers of Adefovir Dipivoxil as a potential liver targeting: Estimation of liver function panel and uptake following intravenous injection of radioiodinated indicator.
المؤلفون: Abd El-Halim SM; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Central Axis, 6th of October City, Giza, 12585, Egypt. shady_mohammed@o6u.edu.eg., Abdelbary GA; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt., Amin MM; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt., Zakaria MY; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy and Pharmaceutical Industry, Port Said University, Port said, 42526, Egypt., Shamsel-Din HA; Department of Labeled Compounds, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo, 13759, Egypt., Ibrahim AB; Department of Labeled Compounds, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo, 13759, Egypt.
المصدر: Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences [Daru] 2020 Dec; Vol. 28 (2), pp. 517-532. Date of Electronic Publication: 2020 Jun 20.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Springer International Publishing Country of Publication: Switzerland NLM ID: 101125969 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 2008-2231 (Electronic) Linking ISSN: 15608115 NLM ISO Abbreviation: Daru Subsets: MEDLINE
أسماء مطبوعة: Publication: 2018- : Cham : Springer International Publishing
Original Publication: Tehran, Iran : The Faculty
مواضيع طبية MeSH: Adenine/*analogs & derivatives , Chemical and Drug Induced Liver Injury/*drug therapy , Liver/*physiopathology , Organophosphonates/*pharmacokinetics , Rose Bengal/*administration & dosage , Thioacetamide/*adverse effects, Adenine/administration & dosage ; Adenine/pharmacokinetics ; Administration, Oral ; Animals ; Chemical and Drug Induced Liver Injury/physiopathology ; Drug Stability ; Injections, Intravenous ; Iodine Radioisotopes/chemistry ; Lipids ; Liver/drug effects ; Liver Function Tests ; Mice ; Nanoparticles ; Organophosphonates/administration & dosage ; Particle Size ; Rose Bengal/chemistry
مستخلص: Purpose: Adefovir dipivoxil (AD), a nucleoside reverse transcriptase inhibitor is effective against Hepatitis B virus. Its poor oral bioavailability leads to frequent administration causing severe adverse effects. Thereby the entrapment of AD within lipid nanoparticulate systems is a way of increasing AD oral bioavailability as a result of improving intestinal permeability with efficient liver-targeted delivery together with higher drug stability during storage.
Methods: AD-loaded nanostructured lipid carriers (AD-NLCs) were prepared via solvent emulsification diffusion technique adopting 2 4 full factorial design to study the effect of lipid percentage, presence of egg yolk lecithin, surfactant type and percentage on entrapment efficiency (E.E.%), particle size and percent in-vitro drug released after 8 h (Q8hrs).
Results: Formula (F12) showed E.E.% of 90.5 ± 0.2%, vesicle size of 240.2 ± 2.5 nm and Q8hrs of 58.55 ± 9.4% was selected as the optimum formula with desirability value of 0.757 based on highest EE%, lowest P.S. and Q8hrs. Further evaluation of the optimized formula using radioiodinated rose bengal (RIRB) in thioacetamide induced liver damage in Swiss Albino mice revealed a higher liver uptake of 22 ± 0.01% ID/g (percent injected dose/g organ) and liver uptake/Blood (T/B) ratio of 2.22 ± 0.067 post 2 h of I.V injection of RIRB compared to 9 ± 0.01% ID/g and 0.64 ± 0.017 in untreated group, respectively.
Conclusion: NLCs could be successfully used as oral drug delivery carriers of the antiviral drug Adefovir Dipivoxil to the liver with higher stability and oral bioavailability. Graphical abstract.
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فهرسة مساهمة: Keywords: Adefovir dipivoxil; Biodistribution study; Nanostructured lipid carrier; Radioiodinated rose bengal; Thiocetamide induced liver damage
المشرفين على المادة: 0 (Iodine Radioisotopes)
0 (Iodine-131)
0 (Lipids)
0 (Organophosphonates)
075T165X8M (Thioacetamide)
1ZPG1ELY14 (Rose Bengal)
JAC85A2161 (Adenine)
U6Q8Z01514 (adefovir dipivoxil)
تواريخ الأحداث: Date Created: 20200622 Date Completed: 20210827 Latest Revision: 20210827
رمز التحديث: 20240829
مُعرف محوري في PubMed: PMC7704840
DOI: 10.1007/s40199-020-00355-8
PMID: 32564282
قاعدة البيانات: MEDLINE
الوصف
تدمد:2008-2231
DOI:10.1007/s40199-020-00355-8