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Development and Evaluation of in-situ Nasal Gel Formulations of Nanosized Transferosomal Sumatriptan: Design, Optimization, in vitro and in vivo Evaluation

Authors Omar MM, Eleraky NE, El Sisi AM, Ali Hasan O

Received 17 October 2019

Accepted for publication 5 December 2019

Published 27 December 2019 Volume 2019:13 Pages 4413—4430


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Editor who approved publication: Dr Yan Zhu

Mahmoud M Omar,1,2 Nermin E Eleraky,3 Amani M El Sisi,4 Omiya Ali Hasan1,2

1Department of Pharmaceutics and Industrial Pharmacy, Deraya University, El-Minia, Egypt; 2Department of Pharmaceutics, Sohag University, Sohag, Egypt; 3Faculty of Pharmacy, Assiut University, Assiut, Arab Republic of Egypt; 4Department of Pharmaceutics and Industrial Pharmacy, Beni-Suef University, Beni-Suef, Egypt

Correspondence: Mahmoud M Omar
Pharmaceutics and Industrial Department, Deraya University, Deraya Square Street, Minia, New-Minia 61768, Egypt
Tel +20 10 0933 2419

Background: Sumatriptan succinate (SUT) is a potent drug used for relieving or ending migraine and cluster headaches. SUT bioavailability is low (15%) when it is taken orally owing to its gastric breakdown and bloodstream before reaching the target arteries.
Aim: The aim of the study was to enhance SUT bioavailability through developing an intranasal transferosomal mucoadhesive gel.
Methods: SUT-loaded nanotransferosomes were prepared by thin film hydration method and characterized for various parameters such as vesicle diameter, percent entrapment efficiency (%EE), in vitro release and ex vivo permeation studies. The in-situ gels were prepared using various ratios of poloxamer 407, poloxamer 188, and carrageenan and characterized for gelation temperature, mucoadhesive strength, and rheological properties.
Results: The prepared transferosomes exhibited percent entrapment efficiencies (%EE) of 40.41±3.02 to 77.47±2.85%, mean diameters of 97.25 to 245.01 nm, sustained drug release over 6 hours, and acceptable ex vivo permeation findings. The optimum formulae were incorporated into poloxamer 407 and poloxamer 188-based thermosensitive in-situ gel using carrageenan as a mucoadhesive polymer. Pharmacokinetic evaluation showed that the prepared in-situ gel of SUT-loaded nano-transferosomes gave enhanced bioavailability, 4.09-fold, as compared to oral drug solution.
Conclusion: Based on enhancing the bioavailability and sustaining the drug release, it can be concluded that the in-situ gel of SUT-loaded nano-transferosomes were developed as a promising non-invasive drug delivery system for treating migraine.

Keywords: nanotransferosomes, sumatriptan succinate, SUT, thermosensitive in-situ gel and intranasal drug delivery system

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