Abstract

Photostability studies were performed on topical formulations containing the anti-inflammatory drug Nabumetone and an analog newly synthesized in order to achieve better photostability and pharmacokinetic profile. Stability tests, according to the International Conference on Harmonization rules, were applied on ethanol solutions and topical gel formulations of both compounds. The photodegradation profiles were monitored by Multivariate curve resolution applied to the UV spectral data. The inclusion of the compounds in microemulsion was investigated to improve light stability and, at the same time, to ensure a sustained release system for skin delivery. All the formulations in solution, gel, microemulsion, and microemulsion-in-gel were exposed to a forced irradiation of 350 W/m2, corresponding to a 21 kJ/m2 min, for up to 300 min. Photostability increased significantly for both drugs in the liquid microemulsion and microemulsion-in-gel, compared to the ethanol solution and plain gel, reaching a residual drug of 97% and 98% for Nabumetone and analog in microemulsion-in-gel, respectively. Permeation experiments on the microemulsion-in-gel showed a better performance of the analog formulated at 0.2%, compared to the same formulation of Nabumetone at 0.7%. These results highlight the potential of the designed matrices as delayed drug delivery systems along with the use of lower drug doses leading to reduced side effects.

Highlights

  • Nabumetone (4-(6-methoxy-2-naphthyl)butan-2-one) (NA), based on a 2,6-disubstituted naphthyl-alkanone structure, is a non-acidic nonsteroidal anti-inflammatory drug (NSAID) which is rapidly metabolized in the liver to the major active metabolite 6-methoxy-2-naphthyl acetic acid (6-MNA) [1]

  • The samples were very stable, similar size and polydispersity index (PDI) and no sedimentation, creaming or flocculation were observed for 6 months

  • The anti-inflammatory drug Nabumetone, through tests defined by international rules, has been confirmed to undergo extensive photodegradation in both solution and gel formulation

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Summary

Introduction

Nabumetone (4-(6-methoxy-2-naphthyl)butan-2-one) (NA), based on a 2,6-disubstituted naphthyl-alkanone structure, is a non-acidic nonsteroidal anti-inflammatory drug (NSAID) which is rapidly metabolized in the liver to the major active metabolite 6-methoxy-2-naphthyl acetic acid (6-MNA) [1]. It seems necessary to develop new strategies aimed at preventing or minimizing photodegradation of NA, considering that the use of protective containers or packaging has proved to be insufficient to guarantee light stability [7,8,9]. NA, considering that the use of protective containers or packaging has proved to be insufficient to guarantee light stability [7,8,9]

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