Development and optimization of Guggul extract loaded ultra-deformable vesicles using central composite design for improving anti-oxidant potential

IF 0.3 Q4 PHARMACOLOGY & PHARMACY Current Drug Therapy Pub Date : 2023-01-16 DOI:10.2174/1574885518666230116103000
Vineet Mittal, Neha Dhankar, R. Verma, Manish Kumar, Anil Hooda, Deepak Kaushik
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Abstract

After almost 30 years of study, it is a scientific fact that inflammation is the root cause of arthritis. Guggul has a beneficial role in arthritis because of its ability to neutralize the NF-kappa factor. A topical drug delivery system is beneficial to overcome the problems associated with oral drug delivery and offers several potential advantages. Ultra-deformable vesicles (UDVs) are a special type of liposome made up of phospholipids and surfactants, and they are highly flexible.Guggul has a beneficial role in arthritis because of its ability to neutralize the NF-kappa factor. A topical drug delivery system is beneficial to overcome the problems associated with oral drug delivery and offers several potential advantages. Ultra-deformable vesicles (UDVs) are a special type of liposome made up of phospholipids and surfactants, and they are highly flexible. In the present investigation, 20 formulations were suggested by Design Expert® 10 software (Central Composite Design) which were prepared using film hydration method with lecithin (70-90 mg), tween 80 (10–30 mg), Guggul extract (3 mg) and sonicated for 5–15 minutes. The formulation was optimized based on particle size (R₁) and maximum entrapment efficiency (R2). The optimized formulation consists of 78.92 mg soya phosphatidyl choline (lecithin), 22.08 mg Tween 80, and 3 mg Guggul with a sonication time of 12.74 minutes that resulted in a particle size of 375.5 ±15.1 nm and entrapment efficiency of 80.3 ± 3.1%. Guggul UDVs showed more antioxidant activity compared to Guggul extract, control and standard. The same results were obtained in the case of anti-arthritic activity, which was measured by egg albumin denaturation, bovine serum albumin denaturation, proteinase inhibitory action, and anti-lipoxygenase activity. The data of both activities were analyzed using an unpaired t-test to determine significant values (p < 0.05). These results demonstrate the potential of UDVs in the treatment of all arthritis diseases.
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利用中心复合设计开发和优化Guggul提取物负载的超变形囊泡以提高抗氧化能力
经过近30年的研究,炎症是关节炎的根本原因是一个科学事实。Guggul在关节炎中具有有益的作用,因为它能够中和NF-κ因子。局部给药系统有利于克服与口服给药相关的问题,并提供了几个潜在的优点。超变形囊泡(UDVs)是一种由磷脂和表面活性剂组成的特殊类型的脂质体,具有高度的柔韧性。Guggul在关节炎中具有有益的作用,因为它能够中和NF-κ因子。局部给药系统有利于克服与口服给药相关的问题,并提供了几个潜在的优点。超变形囊泡(UDVs)是一种由磷脂和表面活性剂组成的特殊类型的脂质体,具有高度的柔韧性。在本研究中,Design Expert®10软件(Central Composite Design)提出了20种配方,这些配方使用卵磷脂(70-90 mg)、吐温80(10-30 mg)、古古尔提取物(3 mg)的膜水合法制备,并超声处理5-15分钟。配方基于颗粒大小(R₁) 和最大包封效率(R2)。优化的配方由78.92 mg大豆磷脂酰胆碱(卵磷脂)、22.08 mg吐温80和3 mg谷朊组成,超声处理时间为12.74分钟,粒径为375.5±15.1 nm,包封效率为80.3±3.1%。与谷朊提取物、对照品和标准品相比,谷朊UDVs表现出更高的抗氧化活性。在抗关节炎活性的情况下获得了相同的结果,其通过鸡蛋白蛋白变性、牛血清白蛋白变性、蛋白酶抑制作用和抗脂氧合酶活性来测量。使用非配对t检验对两种活性的数据进行分析,以确定显著值(p<0.05)。这些结果证明了UDVs在治疗所有关节炎疾病中的潜力。
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来源期刊
Current Drug Therapy
Current Drug Therapy PHARMACOLOGY & PHARMACY-
CiteScore
1.30
自引率
0.00%
发文量
50
期刊介绍: Current Drug Therapy publishes frontier reviews of high quality on all the latest advances in drug therapy covering: new and existing drugs, therapies and medical devices. The journal is essential reading for all researchers and clinicians involved in drug therapy.
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