Comparison of Modern In Vitro Permeability Methods with the Aim of Investigation Nasal Dosage Forms.

Csilla Bartos,Patrícia Varga,Tamás Horváth,Rita Ambrus,Piroska Szabó-Révész

doi:10.3390/pharmaceutics13060846

Abstract

Nowadays, the intranasal route has become a reliable alternative route for drug administration to the systemic circulation or central nervous system. However, there are no official in vitro diffusion and dissolution tests especially for the investigation of nasal formulations. Our main goal was to study and compare a well-known and a lesser-known in vitro permeability investigation method, in order to ascertain which was suitable for the determination of drug permeability through the nasal mucosa from different formulations. The vertical diffusion cell (Franz cell) was compared with the horizontal diffusion model (Side-Bi-Side). Raw and nanonized meloxicam containing nasal dosage forms (spray, gel and powder) were tested and compared. It was found that the Side-Bi-Side cell was suitable for the investigation of spray and powder forms. In contrast, the gel was not measurable on the Side-Bi-Side cell; due to its high viscosity, a uniform distribution of the active substance could not be ensured in the donor phase. The Franz cell, designed for the analysis of semi-solid formulations, was desirable for the investigation of nasal gels. It can be concluded that the application of a horizontal cell is recommended for liquid and solid nasal preparations, while the vertical one should be used for semi-solid formulations.

Highlights

Academic Editors: Paolo Giunchedi and Remigius U
The results showed a steady increase in concentration and a lower permeated amount of MX compared with the results measured on the SideBi-Side system
The aim of this research was to compare the applicability of two diffusion models for permeability investigations of different intranasal formulations

Summary

Introduction

Academic Editors: Paolo Giunchedi and Remigius U. Intranasal administration is an effective way to deliver drugs into the systemic circulation or brain tissues as an alternative to the oral and parenteral routes for some therapeutic agents [1,2]. The intranasal application of nonsteroidal anti-inflammatory drugs (NSAIDs) may be an alternative route for acute pain therapy or to enhance analgesia. Meloxicam- (MX; a poorly water soluble NSAID) containing formulations were developed, intended for intranasal administration. The bioavailability of MX was increased by decreasing its particle size [5,6,7]. In the design of an intranasal powder or suspension as a drug delivery system, it is important to consider the requirement for the particle size of the product (from 5 to 40 μm) [8]

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