Formulation and characterization of a paediatric nanoemulsion dosage form with modified oral drug delivery system for im
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MRS Advances © 2018 Materials Research Society DOI: 10.1557/adv.2018.320
Formulation and characterization of a paediatric nanoemulsion dosage form with modified oral drug delivery system for improved dissolution rate of nevirapine Tapiwa E. Manyarara*1, Star Khoza2, Admire Dube3 and Chiedza C. Maponga1 1
School of Pharmacy, College of Health Sciences, PO BOX MP 167, University of Zimbabwe.
2 Department of Clinical Pharmacology, College of Health Sciences, University of Zimbabwe, P.O. Box A178, Avondale, Harare, Zimbabwe.
3
School of Pharmacy, University of Western Cape, Robert Sobukwe Road, Bellville, 7535, South Africa.
Corresponding author: Mr T. Manyarara: School of Pharmacy, College of Health Sciences, PO BOX MP 167, University of Zimbabwe, Email address: [email protected]
ABSTRACT
Background: The development of appropriate dosage forms for paediatric antiretroviral therapy is key for improved therapeutic outcomes in children. The focus of this study was to improve solubility, dissolution rate, drug release and maintain high drug permeability.
Methodology: A nanoemulsion was prepared using emulsion inversion point and evaluated. The nanoemulsion had nevirapine (3% w/w). In vitro drug release studies were performed using dialysis membrane. Permeability studies using the Caco-2 cell model were performed for the formulation.
Results: The optimized nevirapine nanoemulsion had a mean droplet size of 36.09±12.27nm, low pdI of 0.598 and zeta potential of -7.87±4.35mV. At pH 2, the nanoemulsion released 76 ± 2 % of nevirapine within 2 h, while at pH 6.4 value representing the small intestine, amount of nevirapine released was 41.6± 4 %. The permeability rate of the nevirapine nanoemulsion was 30.02 x 10-6cm/s and higher than that of propranolol. Efflux ratio was 0.02 indicating low chance of drug efflux occurring.
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Conclusion: The results showed that a modified liquid drug release formulations of nevirapine could improve rate of dissolution and maintain high permeability and low drug efflux improving bioavailability of nevirapine in vivo.
INTRODUCTION Drugs that are poorly water soluble represent more than 40% of new chemical entities developed for use on the global pharmaceutical market (1). However, they pose challenges of poor drug absorption, unreliable bioavailability and drug efflux due to physiological mechanisms that exist within the digestive tract (5,6). When drugs exhibit low dissolution rate because of their poor water solubility, they are classified as class II (low solubility and high permeability) or class IV (low solubility and low permeability) according to the Biopharmaceutical Classification System (BCS)(3,4). For BCS class II drugs, the rate limiting step is drug release from the dosage form and solubility in the gastric fluid, so increasing
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