دورية أكاديمية
Enhancement of the bioavailability of an antihypertensive drug by transdermal protransfersomal system: formulation and in vivo study.
| العنوان: | Enhancement of the bioavailability of an antihypertensive drug by transdermal protransfersomal system: formulation and in vivo study. |
|---|---|
| المؤلفون: | Morsi NM; a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Cairo University , Cairo , Egypt and., Aboelwafa AA; a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Cairo University , Cairo , Egypt and., Dawoud MHS; b Department of Pharmaceutics , Faculty of Pharmacy, October University for Modern Sciences and Arts , Dokki , Egypt. |
| المصدر: | Journal of liposome research [J Liposome Res] 2018 Jun; Vol. 28 (2), pp. 137-148. Date of Electronic Publication: 2017 Mar 06. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Informa Healthcare Country of Publication: England NLM ID: 9001952 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1532-2394 (Electronic) Linking ISSN: 08982104 NLM ISO Abbreviation: J Liposome Res Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: London : Informa Healthcare Original Publication: New York, N.Y. : Dekker, c1988- |
| مواضيع طبية MeSH: | Skin Absorption*, Antihypertensive Agents/*pharmacokinetics , Drug Carriers/*chemistry , Drug Compounding/*methods , Timolol/*pharmacokinetics, Administration, Cutaneous ; Administration, Oral ; Animals ; Antihypertensive Agents/administration & dosage ; Antihypertensive Agents/adverse effects ; Biological Availability ; Drug Liberation ; Liposomes/chemistry ; Male ; Nanoparticles/chemistry ; Particle Size ; Phosphatidylcholines/chemistry ; Rats, Wistar ; Skin/metabolism ; Surface Properties ; Surface-Active Agents/chemistry ; Timolol/administration & dosage ; Timolol/adverse effects |
| مستخلص: | Timolol Maleate (TiM), a nonselective β-adrenergic blocker, is a potent highly effective agent for management of hypertension. The drug suffers from poor oral bioavailability (50%) due to its first pass effect and a short elimination half-life of 4 h; resulting in its frequent administration. Transdermal formulation may circumvent these problems in the form of protransfersomes. The aim of this study is to develop and optimize transdermal protransfersomal system of Timolol Maleate by film deposition on carrier method where protransfersomes were converted to transfersomes upon skin hydration following transdermal application under occlusive conditions. Two 2 3 full factorial designs were employed to investigate the influence of three formulation variables which were; phosphatidyl choline: surfactant molar ratio, carrier: mixture and the type of SAA each on particle size, drug entrapment efficiency and release rate. The optimized formulation was evaluated regarding permeation through hairless rat skin and compared with oral administration of aqueous solution on male Wistar rats. Optimized protransfersomal system had excellent permeation rate through shaved rat skin (780.69 μg/cm 2 /h) and showed six times increase in relative bioavailability with prolonged plasma profile up to 72 h. A potential protransfresomal transdermal system was successfully developed and factorial design was found to be a smart tool in its optimization. |
| فهرسة مساهمة: | Keywords: Antihypertensive; design-expert; liposomes; permeation; ultra-flexible vesicles |
| المشرفين على المادة: | 0 (Antihypertensive Agents) 0 (Drug Carriers) 0 (Liposomes) 0 (Phosphatidylcholines) 0 (Surface-Active Agents) 817W3C6175 (Timolol) |
| تواريخ الأحداث: | Date Created: 20170308 Date Completed: 20190207 Latest Revision: 20190215 |
| رمز التحديث: | 20240829 |
| DOI: | 10.1080/08982104.2017.1295989 |
| PMID: | 28264602 |
| قاعدة البيانات: | MEDLINE |
PDF full text from Publisher | تدمد: | 1532-2394 |
|---|---|
| DOI: | 10.1080/08982104.2017.1295989 |