Sains Malaysiana 51(6)(2022): 1861-1873

http://doi.org/10.17576/jsm-2022-5106-21

Fusidic Acid/Tea-Tree Oil Nanoemulsions: A Potentially Safe and Effective Anti MRSA/MSSA Topical Agent for Chronic Wound Healing

(Nanoemulsi Asid Fusidik/Minyak Tea Tree: Agen Topikal Anti MRSA/MSSA yang Berpotensi Selamat dan Berkesan untuk Penyembuhan Luka Kronik)

AHMED YASEEN¹, MOWAFAQ MOHAMMED GHAREEB², DANIA F. ALSAFFAR¹, THAIGARAJAN PARUMASIVAM¹, SEOK-MING TOH¹ & AMIRAH MOHD GAZZALI^1,*

¹School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 USM, Penang, Malaysia

²Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Iraq

Received: 11 October 2021/Accepted: 29 November 2021

Abstract

Fusidic acid (FA) is clinically used as an antibacterial agent for the treatment of Gram-positive bacterial infections. It interferes with bacterial protein synthesis, specifically by preventing the translocation of the elongation factor G on the ribosome. In the present work, oil-in-water nanoemulsion (NE) was developed as a carrier for the transdermal delivery of FA. Different oils, surfactants and co-surfactants were screened. The solubility of FA, the emulsifying capacity of the surfactants and phase diagrams for each oil and surfactant mix were constructed. From the analysis, eight stable NE formulations were chosen, and their physicochemical properties were further evaluated. The antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive Staphylococcus aureus (MSSA) were also evaluated, and cytotoxicity was conducted on HS-27 cell line to determine the safety of the formula. It was found that the NE produced from tea tree oil has the most optimal stability with promising antibacterial activity against MRSA as compared to a commercially available product. The safety profile of the NE was also comparable to the commercial product; thus, the formulated FA-NE is promising for clinical use.

Keywords: Fusidic acid; HS-27; MRSA; nanoemulsion; tea tree oil

Abstrak

Asid fusidik (AF) merupakan agen antibakteria yang digunakan untuk rawatan jangkitan bakteriaGram positif. Ia mengganggu proses sintesis protein dalam bakteria, secara khususnya melalui halangan translokasi faktor pemanjangan G pada ribosom. Dalam kajian ini, nanoemulsi minyak-dalam-air (NE) telah dibangunkan sebagai pembawa kepada penghantaran AF melalui laluan transdermal. Pelbagai jenis minyak, surfaktan and surfaktan bersama telah dinilai. Keterlarutan AF dalam eksipien, kapasiti pengemulsian bagi setiap surfaktan dan rajah fasa telah dibangunkan. Daripada analisis yang dijalankan, lapan formulasi NE yang stabil telah dipilih dan ciri farmakofizikal bagi setiap formulasi ini telah dinilai. Aktiviti antibakteria formulasi-formulasi NE terhadap bakteria Staphylococcus aureus rintang metisilin (MRSA) dan Staphylococcus aureus rentan metisilin (MSSA) juga telah dinilai dan kesan kesitotoksikan telah diuji pada sel HS-27 untuk menentukan keselamatan formula. NE yang dihasilkan daripada minyak tea tree ditemui mempunyai kestabilan yang paling optimum berbanding NE yang dihasilkan daripada minyak lain yang diuji, dengan aktiviti antibakteria yang baik terhadap bakteria MRSA berbanding produk komersial. Keselamatan formula NE juga adalah setara dengan produk komersial, jadi ia berpotensi untuk dibangunkan dengan lebih lanjut bagi kegunaan klinikal.

Kata kunci: Asid fusidik; HS-27; minyak tea tree; MRSA; nanoemulsi

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^*Corresponding author; email: amirahmg@usm.my