Preclinical study on camellia sinensis extract-loaded nanophytosomes for enhancement of memory-boosting activity: optimization by central composite design

IF 3.4 Q2 PHARMACOLOGY & PHARMACY
Varsha Mane, Suresh Killedar, Harinath More, Harshal Tare
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引用次数: 0

Abstract

Background

The purpose of the present study was to enhance the memory-boosting activity of the standardized hydroalcoholic Camellia sinensis extract (CSE) by the formation of nanophytosomes with Leciva S70 phospholipid. The central composite design was used to optimize the solvent evaporation method for the formulation of C. sinesis phytosomes (CSP).

Results

The optimized formulation had a mean particle size of 212.3 nm ± 0.39, PDI of 0.238 ± 0.0197, and zeta potential of −42.02 ± 0.995 mV. C. sinensis phytosome formation was confirmed by analytical techniques. The aqueous solubility of the developed CSP was 95.92 ± 0.31, which is 7.34 times greater than that of pure CSE (13.07 ± 0.19). CSP was found more effective than either pure CSE (26.42 ± 0.4654%) or the physical mixture (32.15 ± 0.4596%) in releasing the CSE from the formulation (72.16 ± 0.5248%). Acute toxicity study corroborated the safety of CSP in rats. CSP demonstrated a significant (p < 0.05) reduction in escape and transferred latency on both days (15th and 16th) as compared to CSE, indicating the improvement of the memory-boosting activity. Furthermore, CSP-treated rats significantly improved acetylcholine (Ach) levels and brain tissue concentration compared with CSE. Moreover, the phytosomal formulation of CSP exhibited its rationality with an improvement of bioavailability by 3.21 folds compared with pure CSE.

Conclusion

The presence of phospholipids in the CSP formulation and the formation of smaller particles may aid in crossing the blood–brain barrier, increasing brain tissue concentration and bioavailability. This, in turn, leads to an increase in memory-boosting activity.

Graphical abstract

山茶提取物载体纳米叶绿体增强记忆促进活性的临床前研究:通过中心复合设计进行优化
背景 本研究的目的是通过与Leciva S70磷脂形成纳米植物体来提高标准化水醇山茶提取物(CSE)的记忆促进活性。结果优化后的配方平均粒径为212.3 nm ± 0.39,PDI为0.238 ± 0.0197,zeta电位为-42.02 ± 0.995 mV。分析技术证实了 C. sinensis 植物胶囊的形成。所开发的 CSP 的水溶性为 95.92 ± 0.31,是纯 CSE(13.07 ± 0.19)的 7.34 倍。与纯 CSE(26.42 ± 0.4654%)或物理混合物(32.15 ± 0.4596%)相比,CSP 能更有效地从制剂中释放 CSE(72.16 ± 0.5248%)。急性毒性研究证实了 CSP 对大鼠的安全性。与 CSE 相比,CSP 在第 15 天和第 16 天的逃逸和转移潜伏期均有显著降低(p < 0.05),这表明 CSP 提高了大鼠的记忆活性。此外,与 CSE 相比,CSP 处理的大鼠乙酰胆碱(Ach)水平和脑组织浓度均有明显改善。此外,与纯 CSE 相比,CSP 植物体制剂的生物利用率提高了 3.21 倍,显示出其合理性。图解摘要
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来源期刊
自引率
0.00%
发文量
44
审稿时长
23 weeks
期刊介绍: Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.
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