Development And Evaluation of In-Situ Nasal Gel Formulations of Nanosized Transferosomal Triptans
Keywords:
Novel drug delivery, transferosomes, in-situ gel, Nasal drug delivery systemAbstract
The study's goal was to create an intranasal transferosomal mucoadhesive gel that would increase the bioavailability of zolmitriptan. Reverse phase evaporation was used to create zolmitriptin-loaded transferosomes, which were then characterised for a number of factors, including vesicle diameter, percent entrapment efficiency (%EE), and in vitro release. Carrageenan, poloxamer 188, and carbopol 934 were used in different ratios to create the in-situ gels, which were then evaluated for rheological characteristics, mucoadhesive strength, and gelation temperature. The produced transferosomes showed sustained drug release over 8 hours, mean diameters of 213.7 ± 1.56 to 508.5 ± 3.75, and percent entrapment efficiencies (%EE) ranging from 49.2 ± 1.24 to 94.3 ± 3.87. Using carrageenan as a mucoadhesive polymer, the best formulae were added to Carbopol 934, poloxamer 188, and carrageenan-based in-situ gel. The in-situ gel of zolmitriptan-loaded nano-transferosomes was created as a promising non-invasive drug delivery method based on improving the bioavailability and drug release
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Choi H-G, Jung J-H, Ryu J-M, Yoon S-J, Oh Y-K, Kim C-K. Development of in situ-gelling and mucoadhesive acetaminophen liquid suppository. Int J Pharm. 1998;165(1):33–44. doi:10.1016/ S0378-5173(97)00386-4
Vishvakrama P, Sharma S. Liposomes: an overview. Journal of Drug Delivery and Therapeutics. 2014 Jun 24:47-55.
Vishvakarma P. Design and development of montelukast sodium fast dissolving films for better therapeutic efficacy. Journal of the Chilean Chemical Society. 2018 Jun;63(2):3988-93.
Vishvakarma P, Mandal S, Verma A. A review on current aspects of nutraceuticals and dietary supplements. International Journal of Pharma Professional’s Research (IJPPR). 2023;14(1):78-91.
Prabhakar Vishvakarma, Jaspreet Kaur, Gunosindhu Chakraborthy, Dhruv Kishor Vishwakarma, Boi Basanta Kumar Reddy, Pampayya Thanthati, Shaik Aleesha, Yasmin Khatoon. Nephroprotective Potential of Terminalia Arjuna Against Cadmium-Induced Renal Toxicity by In-Vitro Study. J. Exp. Zool. India Vol. 28, No. 1, pp. 939-944, 2025
Prabhakar V, Agarwal S, Chauhan R, Sharma S. Fast dissolving tablets: an overview. International Journal of Pharmaceutical Sciences: Review and Research. 2012;16(1):17
Kamel R, Basha M, Abd El-Alim S. Development of a novel vesicular system using a binary mixture of sorbitan monostearate and polyethylene glycol fatty acid esters for rectal delivery of rutin. J Liposome Res. 2013; 23:28–36. doi:10.3109/08982104.2012.727422
Gonza´lez-Rodrı´guez M, Arroyo C, Co´zar-Bernal M, et al. Deformability properties of timolol-loaded transferosomes based on the extrusion mechanism. Statistical optimization of the process. Drug Dev Ind Pharm. 2016; 42:1683–1694. doi:10.3109/03639045. 2016.1165691
Prabhakar V, Agarwal S, Chauhan R, Sharma S. Fast dissolving tablets: an overview. International Journal of Pharmaceutical Sciences: Review and Research. 2012;16(1):17
Vishvakarma P, Mandal S, Pandey J, Bhatt AK, Banerjee VB, Gupta JK. An Analysis of The Most Recent Trends In Flavoring Herbal Medicines In Today's Market. Journal of Pharmaceutical Negative Results. 2022 Dec 31:9189-98
Mostafa DA, Hashad AM, Abdelreheem AYM. Formulation and evaluation of novel brain targeting drug loaded in lipid-based nanoparticles through the intranasal route for Alzheimer. Int Res J Pharm 2019;10:21-7.
Lappin G, Shishikura Y, Jochemsen R, et al. Comparative pharmacokinetics between a microdose and therapeutic dose for clarithromycin, sumatriptan, propafenone, paracetamol (acetaminophen), and phenobarbital in human volunteers. Eur J Pharm Sci. 2011;43 (3):141–150. doi:10.1016/j.ejps.2011.04.009
Dora CP, Singh SK, Kumar S, Datusalia AK, Deep A. Development and characterization of nanoparticles of glibenclamide by solvent displacement method. Acta Pol Pharm. 2010;283–90:283–290.
Gupta M, Goyal AK, Paliwal SR, Paliwal R, Mishra N, Vaidya B, Dube D, Jain SK, Vyas SP. Development and characterization of effective topical liposomal system for localized treatment of cutaneous candidiasis. J Liposome Res. 2010;20:341-350.
Opatha SAT, Titapiwatanakun V, Chutoprapat R. Transfersomes: a promising nanoencapsulation technique for transdermal drug delivery. Pharmaceutics. 2020;12:855.
Cevc G, Schätzlein A, Blume G. Transdermal drug carriers: Basic properties, optimization and transfer efficiency in the case of epicutaneously applied peptides. J Control Release. 1995;36:3-16.
Jangdey MS, Gupta A, Saraf S, Saraf S. Development and optimization of apigenin-loaded transfersomal system for skin cancer delivery: in vitro evaluation. Artif Cells Nanomed Biotechnol. 2017;45:1452-1462.
Kassem MA, Aboul-Einien MH, El Taweel MM. Dry gel containing optimized felodipine-loaded transferosomes: a promising transdermal delivery system to enhance drug bioavailability. AAPS PharmSciTech. 2018;19:2155-2173.
El Zaafarany GM, Awad GA, Holayel SM, Mortada ND. Role of edge activators and surface charge in developing ultradeformable vesicles with enhanced skin delivery. Int J Pharm. 2010;397:164-172.
Maji R, Omolo CA, Jaglal Y, Singh S, Devnarain N, Mocktar C, Govender T. A transferosome-loaded bigel for enhanced transdermal delivery and antibacterial activity of vancomycin hydrochloride. Int J Pharm. 2021;607:120990.
Qushawy M, Nasr A, Abd-Alhaseeb M, Swidan S. Design, optimization and characterization of a transfersomal gel using miconazole nitrate for the treatment of candida skin infections. Pharmaceutics. 2018;10:26.
Rodriguez A, Tatter SB, Debinski W. Neurosurgical techniques for disruption of the blood-brain barrier for glioblastoma treatment. Pharmaceutics 2015;7:175–87.
Begunm MY, Gudipati PR. Formulaton and evalution of dasatinib loaded solid lipid nanoparticles. Int J Pharm Pharm Sci 2018;10:15-20.
Vijayan V, Aafreen S, Sakthivel S, Reddy KR. Formulation and characterization of solid lipid nanoparticles loaded Neem oil for topical treatment of acne. J Acute Disease 2013;2:282-6.
Shelke S, Shahi S, Jalalpure S, Dhamecha D. Poloxamer 407-based intranasal thermoreversible gel of zolmitriptan-loaded nanoethosomes: formulation, optimization, evaluation and permeation studies. J Liposome Res 2016;26:313-23.
Bhattacharyya S, Sudheer P, Das K, Ray S. Experimental design supported liposomal aztreonam delivery: in vitro studies. Adv Pharm Bull. 2021;11:651-662.
Kanugo A, Deshpande A, Sharma R. Formulation optimization and evaluation of nanocochleate gel of famciclovir for the treatment of herpes zoster. Recent Pat Nanotechnol. 2023;17:259-269.
Zhang ZJ, Michniak-Kohn B. Flavosomes, novel deformable liposomes for the co-delivery of anti-inflammatory compounds to skin. Int J Pharm. 2020;585:119500.
Bhattacharyya S. Statistical optimization amalgamated approach onBformulation development of nano lipid carrier loaded hydrophilic gel of fluticasone propionate. Indian J Pharm Educ Res. 2021;55:418-427.
Thakur N, Jain P, Jain V. Formulation development and evaluation of transferosomal gel. J Drug Deliv Ther. 2018;8:168-177.
Rajan R, Vasudevan DT. Effect of permeation enhancers on the penetration mechanism of transfersomal gel of ketoconazole. J Adv Pharm Technol Res. 2012;3:112-116.
Raza A, Ansari TM, Niazi SB. A novel spectrophotometric method for the determination of zolmitriptan in pharmaceutical formulations. J Chin Chem Soc 2007;54:1413-7.
Jain R, Nabar S, Dandekar P, Patravale V. Micellar nanocarriers: potential nose-to-brain delivery of zolmitriptan as novel migraine therapy. Pharm Res 2010;27:655-64.
Shiledar RR, Tagalpallewar AA, Kokare CR. Formulation and in vitro evaluation of xanthan gum-based bilayered mucoadhesive buccal patches of zolmitriptan. Carbohydr Polym 2014;101:1234-42.
Bayrak Z, Tas C, Tasdemir U, Erol H, Ozkan CK, Savaser A, et al. Formulation of zolmitriptan sublingual tablets prepared by direct compression with different polymers: in vitro and in vivo evaluation. Eur J Pharm Biopharm 2011;78:499-505..
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