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Intranasal spray of cubosomal Tizanidine Hydrochloride for brain targeting: In-vitro and in-vivo characterization.

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Tizanidine HCl (TH) is used as first-line therapy for the treatment of muscular spasm. The intranasal cubosomal delivery system of TH for site-specific delivery i.e. CNS was developed. Cubosomes of… Click to show full abstract

Tizanidine HCl (TH) is used as first-line therapy for the treatment of muscular spasm. The intranasal cubosomal delivery system of TH for site-specific delivery i.e. CNS was developed. Cubosomes of TH were prepared using Glyceryl monooleate (GMO) as a lipid, poloxamer 407 as stabilizer, and ethanol and polyethylene glycol 200 as co-solvent. Optimized cubosomes of TH were characterized for vesicle size, zeta potential, % drug entrapment, mucin binding efficiency, which found to be 50.22 nm, -6.39 mV, 69.28%, 42.12%. It is also evaluated for CRYO-FESEM, CRYO-TEM, SAXS, residual solvent content, and in-vitro drug release. Ex-vivo permeation was also conducted at 7.4 and it indicates that almost 93.66% drug was diffused from a formulation in 6 hrs. Histopathological study of the optimized TH cubosomes suggests that the prepared formulation is non-toxic to the nasal mucosa. Pharmacokinetic and brain distribution study indicates targeted action of the formulated TH cubosomes.

Keywords: intranasal spray; vivo; brain; spray cubosomal; tizanidine; intranasal

Journal Title: Journal of microencapsulation
Year Published: 2023

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