Preparation and Evaluation of 5-Florouracil loaded Nano-Structured lipid carrier by double emulsification techniques

Saripadiya Nimesh D, D. M. M. Patel
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Abstract

Skin cancer remains the second most common cancer causing death in majority of the population worldwide.” Chemotherapeutical treatment generally includes treatment by administration of chemotherapeutical formulations mostly by intravenous route of administration which is painful, toxic, time consuming and costly for the patients. Chemotherapy also causes toxicity and cell death to other normal cells in the body apart from cancerous cells. The aim of the present investigation was to formulate a topical nano-particulate drug delivery system which causes lower exposure to normal body cells by higher efficacy of targeting the cancerous cells, producing lower toxicity rates and avoiding maximum possible side effects.” “Henceforth, an anti-neoplastic agent has been used in order to prepare Nano-structured Lipid Carriers (NLCs) which was further loaded into gel formulation for topical application. “The nano-structured lipid carrier (NLCs) of 5-fluorouracil (5-FU) were prepared by using Compritol ATO 888 by double emulsification method.” The lipids were selected based on the solubility studies and partition coefficient of 5-FU in lipids. The particle size of optimized formulation was found to be 246.2nm. The in vitro release studies of developed NLCs was carriers carried out at pH 7.4. Sodium carboxy methylcellulose, hydroxyl propyl methyl cellulose , and chitosan hydrogels loaded with NLCs were developed. The permeability behavior through dialysis membrane was performed for 24 hrs and Q 24 of optimized gel formulation was found to be 435.974µg/cm 2 .The steady-state flux (Jss) was found to be 0.062102 mg/cm 2 , and permeability coefficient (Kp) was found to be 4.14013 cm/hr for optimized NLCs based gel formulation for ex-vivo skin permeability studies.
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双乳化法制备5-氟尿嘧啶纳米结构脂质载体及评价
皮肤癌仍然是全球大多数人口中导致死亡的第二大常见癌症。”化疗治疗一般包括化疗制剂的治疗,主要是通过静脉给药,这对患者来说是痛苦的、有毒的、耗时的和昂贵的。化疗也会对身体中除癌细胞外的其他正常细胞造成毒性和细胞死亡。本研究的目的是研制一种局部纳米颗粒药物递送系统,通过更高的靶向癌细胞的效率,减少对正常细胞的暴露,产生更低的毒性率,并避免最大可能的副作用。“此后,一种抗肿瘤药物被用于制备纳米结构脂质载体(nlc),并被进一步装载到凝胶配方中用于局部应用。”采用双乳化法制备了5-氟尿嘧啶(5-FU)纳米结构脂质载体(NLCs)。根据脂质中5-FU的溶解度研究和分配系数选择脂质。优化后的配方粒径为246.2nm。开发的NLCs体外释放研究是在pH 7.4的条件下进行的。制备了羧甲基纤维素钠、羟丙基甲基纤维素和壳聚糖水凝胶。通过透析膜渗透24小时,优化后的凝胶配方q24为435.974µg/ cm2,稳态通量(Jss)为0.062102 mg/ cm2,渗透系数(Kp)为4.14013 cm/hr。
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