• Document: Self-Nanoemulsifying Drug Delivery Systems of Poorly Soluble Drug Dutasteride: Formulation and In-Vitro characterization
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Journal of Applied Pharmaceutical Science Vol. 7 (04), pp. 011-022, April, 2017 Available online at http://www.japsonline.com DOI: 10.7324/JAPS.2017.70402 ISSN 2231-3354 Self-Nanoemulsifying Drug Delivery Systems of Poorly Soluble Drug Dutasteride: Formulation and In-Vitro characterization Poonguzhali Subramanian, Rajinikant Siddalingam* School of Pharmacy, Taylor’s University Lakeside Campus, Kualal Lumpur, Malaysia. ARTICLE INFO ABSTRACT Article history: The present study aims to prepare and evaluate the self-nanoemulsifying drug delivery system (SNEDDS) to Received on: 30/08/2016 enhance the dissolution rate of a poorly soluble drug dutasteride. The formulation was prepared using capryol Accepted on: 18/12/2016 PGMC, Cremophor EL, and polyethylene glycol (PEG) 400 as oil, surfactant and co-surfactant, respectively. Available online: 30/04/2017 The pseudo-ternary phase diagrams with presence and absence of drug were plotted to find out the nanoemulsification range and also to evaluate the effect of dutasteride on the emulsification behavior of the Key words: phases. Prepared SNEDDS formulations were evaluated for its particle size distribution, nanoemulsifying Self emulsifying Drug properties, robustness to dilution, self-emulsification time, turbidity measurement, drug content and in-vitro Delivery System, dissolution. Furthermore, the optimized formulations were evaluated for heating cooling cycle, centrifugation Dutasteride, Poorly soluble studies, freeze thaw cycling, particle size distribution and zeta potential to confirm the stability of the formed drug, Nanoemulsions, SNEDDS formulations. The particle size, zeta potential and polydispersity index of the optimized formulation Enhancement of dissolution. was found to be 35.45 nm, -15.45 and 0.19, respectively. The in vitro results revealed that the prepared formulation enhanced the dissolution rate of dutasteride significantly compared to pure drug. In 60 minutes, the formulation showed 83.15% and 82.04 % drug release for pH 6.8 and pH 1.2 respectively. Based on the results, it was concluded that the dutasteride-loaded SNEDDS revealed better dissolution compared to the raw drug suspension and commercial drug. INTRODUCTION reductase (5AR), which is responsible for the conversion of Benign prostate hyperplasia (BPH) is the most common testosterone to a more potent dihydrotestosterone (Dolder, 2006). benign neoplasm which approximately 80 % of the elderly men Dutasteride is a drug of choice in the group of inhibitors. Compared (above 60 years old) develops the microscopic evidence of BPH to other 5AR inhibitor such as finasteride, dutasteride is superior as (Dolder, 2006). Among them, half of the patients develop it binds to both types of alpha-reductases: type I 5AR and type II enlarged prostate gland, followed by symptoms such as nocturia, 5AR. Although type I 5AR is mainly active in skin and liver, and its increase in urinary urgency and frequency, and reduced force of inhibition, further, reduces the total circulating DHT (Kim, 2013). stream. For patients with enlarged prostate, the treatment would Dutasteride is 45 times more potent than finasteride to inhibit type 1 be invasive surgery and prostatectomy. Without surgery, the 5AR, and 2.5 times more potent to inhibit type 2 5AR, thus have treatment would be to stop the static factor of prostate gland more significant effect in reducing DHT count (Keam and Scott, enlargement, which is dihydrotestosterone (DHT). DHT is a 2008). In a study carried out by Dolder (2006), dutasteride decreases potent androgen, which is converted from testosterone to DHT by ~95%, as compared to 70% reduction in patient receiving androstenedione. Inhibition of DHT formation can be a treatment finasteride based on a four-year observation. It is a recommended strategy to reduce prostate size. Dutasteride inhibits 5-alpha regimen for benign prostate hyperplasia treatment to improve symptoms. However, being classified as Biopharmaceutical Classification System (BCS) class II or IV, it has poor aqueous * Corresponding Author Rajinikanth Siddalingam, School of Pharmacy, Taylor's university solubi

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