Abstract
Objective: The main objective of the present research work was to develop, optimize, and characterize microemulsion (ME) of frovatriptan succinate to improve brain transport.
 Methods: The pseudoternary phase diagrams were constructed for ME formulations composed of Capmul MCM, Cremophor EL, and propylene glycol. Frovatriptan succinate-loaded ME was optimized by simplex lattice design having the concentration of oil, surfactant, and cosurfactant representing three apex points on the triangle. These were taken as independent variables and percentage drug release as a response variable. All developed batches of ME were characterized for in vitro tests, histopathology study, and pharmacokinetics in Swiss albino rats.
 Results: Clear MEs were obtained. F5 having particle size – 142.0 nm, zeta potential – 17.7–−7.8 mv, refractive index – 1.38±0.20, drug content – 98.24±0.20%, and drug diffused through dialysis membrane – 85% was the optimized batch. Drug permeation through the nasal mucosa of F5 in the ex vivo study was found to be 82.32%. Histopathology microscopic study has shown that F5 does not cause any irritation and structural changes in sheep nasal mucosa. The pharmacokinetic parameters were determined after nasal and oral administration of F5. For brain tissue, after nasal administration were Cmax181±1.51 ng/ml, Tmax – 2±1.01, area under curve (AUC)0−6 – 390.0±2.08 ng.h/ml. The AUC0−6 attained by nasal ME was 3.29 times greater than oral solution. Drug targeting index of frovatriptan succinate was 2.06. This was found satisfactory.
 Conclusion: Microemulsion of said composition was found to be enhancing delivery of frovatriptan succinate to brain tissues through nasal route.
Highlights
The nasal mucosa has been considered as a route of administration to speed up a higher level of drug absorption
This potential lies in the ability of nasal mucosa of high drug permeation due to exceedingly vascularization
Nasal administration minimizes the lag time associated with oral drug delivery and offers non-invasiveness [6]
Summary
The nasal mucosa has been considered as a route of administration to speed up a higher level of drug absorption. Among the mucosal sites in the human body, nasal mucosa has the potential to compete with the intravenous route for fast onset of action and percentage bioavailability [1]. This potential lies in the ability of nasal mucosa of high drug permeation due to exceedingly vascularization. The olfactory region of the nose has the potential to stream a drug to the central nervous system (CNS) [2] This offers the possibility to target CNS by bypassing blood–brain barrier (BBB) [3]. Nasal administration minimizes the lag time associated with oral drug delivery and offers non-invasiveness [6]
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