Abstract
The use of miconazole nitrate (MN) in the treatment of oropharyngeal candidiasis (OPC) is limited by low drug bioavailability, frequent administration, fungal resistance and toxicity concerns. Lipid nanogel comprising solid lipid nanoparticles (SLNs) incorporated into a gel base could be employed to prolong and target MN to the oromucosal layers, minimizing its associated side effects while enhancing its lethality against resistant Candida albicans. In this study, novel tailor-made oropharyngeal lipid nanogels encapsulating MN were developed and evaluated for improved treatment of OPC. Wide angle X-ray diffractogram analysis revealed the amorphous nature of the lipid matrix, containing beeswax and Phospholipon® 90H, used in preparing the SLNs. The SLNs had varied polydispersity indices, good encapsulation efficiency (EE) and mean droplet size of 204.0±2.9–263.0±7.1 nm. The developed lipid nanogels were pseudoplastic and possessed suitable mucoadhesive strengths on ‘cow-everted’ oromucosal tissue, with greater anticandidal properties regarding fungal inhibition than marketed MN formulation (Daktarin® oral gel) at equivalent concentration. This study has shown that the activity of MN against oral thrush swab (OTS) of C. albicans was improved by formulation as tailor-made mucoadhesive lipid nanogel, and hence could be exploited as an alternative therapeutic carrier for the effective treatment of OPC.
About the authors
Franklin C. Kenechukwu is a lecturer at the Department of Pharmaceutics, University of Nigeria, Nsukka, where he studied Pharmacy and obtained his PhD in 2017. He is a 2017 recipient of the Association of Commonwealth Universities early career grant. His research focuses on development and physicochemical characterization of engineered smart nanomedicines for improved topical and transmucosal delivery of bioactives and biomolecules for enhanced treatment of infectious diseases, especially bacterial and fungal infections and vector-borne diseases. Dr. Kenechukwu has published widely in peer-reviewed high impact journals, electronic and printed books and has also attended many conferences.
Anthony A. Attama is a Professor of Pharmaceutics at the University of Nigeria, Nsukka, where he studied Pharmacy and obtained his PhD in 2002. Professor Attama was at the Institut fur Pharmazeutische Technologie, Technische Universitat Braunschweig, Germany for his postdoctoral research in Pharmaceutical Nanotechnology. He is the leader of the Drug Delivery and Nanomedicines Research Group of the University of Nigeria, Nsukka. He supervises postgraduate students and has published widely in peer-reviewed high impact journals. Professor Attama has won many honors and research grants and has also attended many conferences. He has fostered the establishment of some pharmaceutical industries in Nigeria.
Emmanuel C. Ibezim is a Professor in the Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka. His research interests include the interactions between some locally available food materials and commonly used drugs, biotechnology, pharmaceutical raw materials development and quality control of pharmaceuticals. He is the Pioneer Head of the Department of Pharmaceutical Microbiology and Biotechnology, University of Nigeria, Nsukka. He has received many academic and non-academic awards. He is a member of editorial boards for many national and international journals. He has coauthored many books, contributed many book chapters and has many articles published in peer-reviewed journals and has attended many conferences.
Petra O. Nnamani is senior lecturer and holds a PhD in Drug Delivery at the Department of Pharmaceutics, University of Nigeria, Nsukka (UNN). She has had postdoc positions in SUK India (2012) and HIPS Saarland University, Germany (2013). Her research focuses on physicochemical characterization of nano-engineered particles to exploit biological barriers of the GIT and the skin, for sustained action in different disease conditions (e.g. malaria, infections, diabetes, etc.); as well as providing clean safe water for better public health using plant-based super-porous nanomaterials through her Clean Water Group operating under the Public Health & Environmental Sustainability (PHES) Research Group in UNN.
Chukwuebuka E. Umeyor is a lecturer in the Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Nnamdi Azikiwe University, Awka, Nigeria. He obtained his Bachelor of Pharmacy (BPharm) in 2007, Master of Pharmacy (MPharm) in 2010, and Doctor of Philosophy (PhD) all from the University of Nigeria, Nsukka, Enugu State, Nigeria. He has several publications in reputable peer-reviewed local and international journals. His research interest is the use of nanovectors for improved drug delivery.
Emmanuel M. Uronnachi is a graduate of the University of Nigeria, Nsukka, Enugu state, Nigeria, with a PhD in Physical Pharmaceutics (Formulation Science). He currently lectures in the Pharmaceutics and Pharmaceutical Technology Department of Nnamdi Azikiwe University, Awka, Nigeria. His research interests include: enhancing bioavailability of poorly water soluble drugs using different formulation approaches including nanoparticle and microparticle technology; combination therapies for treatment of common tropical diseases; and excipient and API manufacturing. He has authored several articles on drug formulation.
Mumuni A. Momoh is a senior lecturer and holds PhD at the Department of Pharmaceutics, University of Nigeria, Nsukka. His research interests include drug discovery and delivery using biodegradable polymers and lipids. He is very keen on researching alternative routes of insulin delivery, which has won him the prestigious national Tertiary Education Trust Fund (TETFund) scholarship at the University of Nigeria, Nsukka as well as the Matsume post-doctoral scholarship in Japan. Dr. Momoh has won several other honors and research grants and has also attended many conferences. He has coauthored many books, contributed many book chapters and has many articles published in peer-reviewed journals.
Paul A. Akpa holds a PhD in Physical Pharmaceutics from the University of Nigeria, Nsukka. He is currently a senior lecturer in the Department of Pharmaceutics of the University of Nigeria, Nsukka. He has attended international conferences and published papers in both local and international journals. He is interested in novel drug delivery systems.
Acknowledgments
This work makes part of the doctoral activities of Franklin C. Kenechukwu. We thank Phospholipid GmbH, Köln, Germany for providing Phospholipon® 90H (P90H) used in this study. We also acknowledge Lubri-zol Corporation, Ohio, USA for the kind gift of Noveon® (Polycarbophil).
Conflict of interest: The authors state no conflict of interest. All authors have read the journal’s publication ethics and publication malpractice statement available at the journals’ website and hereby confirm that they comply with all its parts applicable to the present scientific work.
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Supplemental Material:
The online version of this article offers supplementary material (https://doi.org/10.1515/ejnm-2017-0010).
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