Topical Delivery of Meloxicam using Liposome and Microemulsion Formulation Approaches.

Julia Zhang,Anna Froelich,Bozena Michniak-Kohn

doi:10.3390/pharmaceutics12030282

Abstract

The aim of this study is to develop, characterize and compare conventional liposome, deformable liposome (transfersome) and microemulsion formulations as potential topical delivery systems for meloxicam. Liposomes were characterized in terms of vesicle size, zeta potential and entrapment efficiency. For microemulsions, particle size, electrical conductivity and viscosity studies were performed to assess the structure of the investigated systems. An ex vivo skin permeation study has been conducted to compare these formulations. The dermal and transdermal delivery of meloxicam using these formulations can be a promising alternative to conventional oral delivery of non-steroidal anti-inflammatory drugs (NSAIDs) with enhanced local and systemic onset of action and reduced side effects.

Highlights

Meloxicam is a non-steroidal anti-inflammatory drug (NSAID) structurally related to the enolic acid class of 4-hydroxy-1,2-benzothiazine carboxamides
In the case of oil in water (o/w) microemulsions, the oil phase might act as a drug reservoir, maintaining a high concentration gradient between the formulation and the skin [22]. We present both liposomal and microemulsion formulations investigated as potential carriers for the dermal delivery of meloxicam
The results indicated that the entrapment efficiency for transfersome incorporating Cetylpyridinium chloride (CPC) (84%) were much higher than that of conventional liposomes

Summary

Introduction

Meloxicam is a non-steroidal anti-inflammatory drug (NSAID) structurally related to the enolic acid class of 4-hydroxy-1,2-benzothiazine carboxamides It was first approved as a 7.5 mg tablet (Mobic; Boehringer Ingelheim) by the United Stated Food and Drug Administration (US FDA) in 2000 and was later approved and marketed in capsule and suspension forms. Meloxicam has been studied as a potential drug for Alzheimer’s disease and as a viable adjuvant therapeutic agent to treat different cancers, such as lung, colorectal, prostate and urinary bladder cancers [1,2,3,4,5] Adverse effects, such as gastro-intestinal toxicity/bleeding, headaches, rash, increased risk of cardiovascular events, etc., are frequently reported when this drug is administrated at high doses and with long-term treatment [6].

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