Formulation and evaluation of cubosomes containing colchicine for transdermal delivery
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ORIGINAL ARTICLE
Formulation and evaluation of cubosomes containing colchicine for transdermal delivery Mohamed Nasr 1,2
&
Hassan Younes 3 & Rania S. Abdel-Rashid 1
# Controlled Release Society 2020
Abstract Gout is a common inflammatory disease that is characterized by the deposition of serum urate crystals in the synovial fluids and joints. In spite of high efficiency of colchicine (COL) in treatment of gout, it has potential side effects associated with its oral administration. This study was aimed to enhance COL bioavailability and minimize associated side effects through transdermal delivery of COL-loaded cubosomes. Eight cubosomal dispersions were prepared according to Box-Behnken factorial design and the effect of COL, glyceryl monooleate (GMO), and surfactant (P407) concentrations on particle size distribution, zeta potential, and entrapment efficiency were assessed. The results revealed that the optimum formula exhibited a mean particle size of 73.07 ± 2.18 nm and entrapped 32.40 ± 2.33% of COL. The influence of transdermal application of COL cubosomal gel on the in vivo absorption of the drug was studied in rats compared with oral COL solution. The results of in vivo study showed that transdermal application of COL cubosomal gel significantly improves the drug absorption compared with oral COL solution, with evidence of a relative bioavailability of 4.6 times greater than that of oral COL solution. In conclusion, transdermal application of COL cubosomal gel may be a promising delivery system for enhancing the bioavailability of COL. Keywords Colchicine . Cubosomes . Bioavailability . Transdermal delivery
Introduction Gout represents one of the most painful medical conditions ever expressed by humans. According to the National Institute of Arthritis and Musculoskeletal Disease, gout has been a serious medical condition prevailing in almost 275 out of every 100,000 people in the world where its prevalence has been doubled in the last 20 years with more than 15.8% of the affected patients being below the age of 30 [1]. Gout is caused by the crystallization and deposition of uric acid within synovial fluids and is associated with increased level of serum uric acid [2]. Treatment of gout includes the use of corticosteroids,
* Mohamed Nasr [email protected] 1
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo 11790, Egypt
2
Department of Pharmaceutics, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa, Egypt
3
Hi Pharm for Manufacturing Pharmaceuticals and Chemicals, Obour, Egypt
NSAIDs, xanthine oxidase inhibitors, and colchicine (COL) [3–7]. COL, a natural extracted alkaloid obtained from Colchicum autumnale L. plant, has been recognized among approaches for management of gouty arthritis [8]. The drug is also used in treatment of several medical conditions such as, Familial Mediterranean fever, psoriasis, and actinic keratosis [9–12]. It is not used as a first-line drug due to its narrow therapeutic window and increased side ef
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