Formulation Variables Effect on Gelation Temperature of Nefopam Hydrochloride intranasal in Situ Gel (Conference Paper) #

Abstract

Nefopam (N.F.) HCl is a non-narcotic centrally-acting, non-opioid benzoxazocine analgesic to relieve acute and chronic pain. It exhibits low bioavailability (about 36%) due to its first-pass degradation in the liver.
 Intranasal administration has been used as a new route for targeting active brain sites and enhancing the bioavailability of N.F. HCl bypassing hepatic metabolism.
 In situ gel of N.F. HCl was prepared by the cold method using different concentrations of Poloxamer 407, Poloxamer 188, HPMC K4M, Carbapol 934, and Hyaluronic acid polymers.
 The results show that identification tests are superimposed with references, solubility study shows that N.F. HCl is suitable to be administered intranasally; Compatibility studies reveal incompatibility of Nefopam HCl with HPMC K4M and Carbapol 934; meanwhile, no interaction with Methylcellulose and Hyaluronic acid.
 In conclusion, the obtained results revealed the incredible ability of the produced N.F. HCl intranasal in situ gel is intended to enhance drug bioavailability bypassing the metabolizing effect of the liver that N.F. HCl is facing when given orally.

Frovatriptan succinate intranasal delivery for brain targeting – in vivo study.‎

“…In situ gelling systems that are ion-activated include gellan gum and sodium alginate, whereas temperaturedependent methods include Pluronics, Tetronics, and polymethacrylates (e.g., Carbopol and cellulose acetate phthalate) (18,43,44). In situ, gels provide several advantages over typical gels, such as being simpler to produce, injectable as a liquid, and able to remain on the surface of the nasal cavity for a longer time owing to gelling (45)(46)(47)(48)(49)(50). In this study, the polymer poloxamer 407 and the mucoadhesive polymer Carbopol 934 were used to develop in situ gel formulations of FVT for intranasal distribution, to extend the drug's residence time in the nasal cavity and enhance its absorption across the nasal-mucosal barrier.…”

Formulation and Characterization of Intranasal Drug Delivery of Frovatriptan-Loaded Binary Ethosomes Gel for Brain Targeting

“…[24][25][26][27][28] In situ, gels provide several advantages over typical gels, such as being simpler to produce, injectable as a liquid, and able to remain on the nasal cavity's surface for a longer time owing to gelling and mucoadhesion. 29,30 The current study aims to prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosomes.…”