Most Cited Article – Curcumin Loaded Ethosomal Gel for Improved Topical Delivery: Formulation, Characterization and Ex-vivo Studies

Author(s):Bhumika Kumar*P.K. Sahoo and Satish Manchanda

Volume 9, Issue 4, 2021

Published on: 08 February, 2021

Page: [281 – 287]

Pages: 7

DOI: 10.2174/2211738509666210208225826

Abstract

Background: Curcumin is a curcuminoid, which is an active constituent of turmeric and is obtained from the rhizomes of Curcuma longa, family Zingiberaceae. Curcumin modulates the activity of various transcription factors and regulates the expression of inflammatory enzymes, cell survival proteins, adhesion molecules and cytokines by binding to a variety of proteins and inhibiting the activity of various kinases. Curcumin falls in the BCS class IV drug, with poor solubility and poor permeability which makes it very challenging to utilize the maximum therapeutic potential of this moiety

Objective: The major aim of the study was to enhance transdermal penetration of curcumin via ethosomal gel and to overcome the barriers of poor permeability of transdermal drug delivery.

Methods: Curcumin loaded ethosomes were prepared with varying quantities of ethanol and soya lecithin by the cold method and were optimised based on entrapment efficiency, vesicular size and Ex-vivo studies. Optimised ethosomal formulation was further incorporated into a gel and was evaluated. Ex-vivo studies were performed with the ethosomal gel of curcumin and was compared with simple drug solution.

Results: Prepared ethosomal system showed a vesicle size ranging from 211 to 320 nm with spherical, smooth surface and entrapment efficiency of 87 to 91%. Optimised ethosomal system (ET3) was incorporated into gel and was further evaluated.

Conclusion: The findings of the research work suggested that the ethosomal gel holds excellent potential for transdermal delivery of curcumin. Read Now: https://bit.ly/3BYYN5A

Article by Disease | Design and Characterization of Mucoadhesive Gelatin-Ethylcellulose Microparticles for the Delivery of Curcumin to the Bladder

Bentham Oncology Collection | Oncology | Bladder Cancer 

 

Graphical Abstract:

 

Abstract:

Background: Bladder cancer is the second type of malignant carcinoma of the urinary tract. The treatment is time-consuming and requires maintenance doses of the drug for long period of time with important side effects. Curcumin has shown evident clinical advances in the treatment of cancer. The technology of microencapsulation and the use of mucoadhesive materials can contribute to modify the delivery and improve the bioavailability of curcumin.

Objective: The aim of this study was to design and characterize mucoadhesive microparticles containing curcumin using multivariate analysis and the spray-drying technique.

Methods: A factorial design 32+1 was employed to investigate the influence of gelatin, ethylcellulose, and curcumin on size, polydispersity index, drug content and entrapment efficiency. Microparticles were also evaluated by ATR-FTIR, X-ray diffraction, antioxidant activity, in-vitro release profile, exvivo mucoadhesion performance, and in-vitro cytotoxicity.

Results: Microparticles showed non-uniform surface, mean diameter from 2.73 µm to 4.62 µm and polydispersity index from 0.72 to 1.09, according to the different combinations of the independent factors. These independent variables also had a significant effect on the drug content. The highest values of drug trapping efficiency were obtained with the highest concentration of curcumin and polymers. Formulations displayed slow drug release and important antioxidant activity. The good mucoadhesive performance of microparticles was assessed by the falling film technique. Moreover, the formulations did not display in vitro toxicity against Artemia salina and Fibroblasts LM(TK).

Conclusion: The design results were useful for developing of curcumin dosage form with good physicochemical characteristics and mucoadhesive properties for the bladder administration.

 

Find out more at: http://www.eurekaselect.com/node/161813/article

EDITOR’S CHOICE – Crystalline Ethylene Oxide and Propylene Oxide Triblock Copolymer Solid Dispersion Enhance Solubility, Stability and Promoting Time- Controllable Release of Curcumin

JOURNAL: Recent Patents on Drug Delivery & Formulation

AUTHOR(S): Thais F.R. Alves, Franciely C.C. das Neves Lopes, Marcia A. Rebelo, Juliana F. Souza, Katiusca da Silva Pontes, Carolina Santos, Patricia Severino, Jose M.O. Junior, Daniel Komatsu, Marco V. Chaud

Graphical Abstract:

 

Abstract:

Aims and Background: The design and development of an effective medicine are, however, often faced with a number of challenges. One of them is the close relationship of drug’s bioavailability with solubility, dissolution rate and permeability. The use of curcumin’s (CUR) therapeutic potential is limited by its poor water solubility and low chemical stability. The purpose was to evaluate the effect of polymer and solid dispersion (SD) preparation techniques to enhance the aqueous solubility, dissolution rate and stability of the CUR. The recent patents on curcumin SD were reported as (i) curcumin with polyvinylpyrrolidone (CN20071 32500 20071214, WO2006022012 and CN20151414227 20150715), (ii) curcumin-zinc/polyvinylpyrrolidone (CN20151414227 20150715), (iii) curcumin-poloxamer 188 (CN2008171177 20080605), (iv) curcumin SD prepared by melting method (CN20161626746-20160801).

Materials and Methods: SD obtained by co-preciptation or microwave fusion and the physical mixture of CUR with Poloxamer-407 (P-407), Hydroxypropylmetylcellulose-K4M (HPMC K4M) and Polyvinylpyrrolidone-K30 (PVP-K30) were prepared at the ratios of 1:2; 1:1 and 2:1. The samples were evaluated by solubility, stability, dissolution rate and characterized by SEM, PXRD, DSC and FTIR.

Results: The solubility, stability (pH 7.0) and dissolution rate were significantly greater for SD (CUR:P-407 1:2). The PXRD,SEM and DSC indicated a change in the crystalline state of CUR. The enhancement of solubility was dependent on a combination of factors including the weight ratio, preparation techniques and carrier properties. The drug release data fitted well with the Weibull equation, indicating that the drug release was controlled by diffusion, polymer relaxation and erosion occurring simultaneously.

Conclusion: Thus, these SDs, specifically CUR:P-407 1:2 w/w, can overcome the barriers of poor bioavailability to reap many beneficial properties.

Read more here: http://www.eurekaselect.com/159171/article

 

 

EDITOR’S CHOICE – Y-shaped Folic Acid-Conjugated PEG-PCL Copolymeric Micelles for Delivery of Curcumin – Anti-Cancer Agents in Medicinal Chemistry

Journal: Anti-Cancer Agents in Medicinal Chemistry

Author(s): Runliang Feng, Wenxia Zhu, Wei Chu, Fangfang Teng, Ning Meng, Peizong Deng, Zhimei Song

Abstract:

Background: Curcumin is a natural hydrophobic product showing anticancer activity. Many studies show its potential use in the field of cancer treatment due to its safety and efficiency. However, its application is limited due to its low water-solubility and poor selective delivery to cancer.

Objective: A Y-shaped folic acid-modified poly (ethylene glycol)-b-poly (ε-caprolactone)2 copolymer was prepared to improve curcumin solubility and realize its selective delivery to cancer.

Method and Results: The copolymer was synthesized through selective acylation reaction of folic acid with α- monoamino poly(ethylene glycol)-b-poly(ε-caprolactone)2. Curcumin was encapsulated into the copolymeric micelles with 93.71% of encapsulation efficiency and 11.94 % of loading capacity. The results from confocal microscopy and cellular uptake tests showed that folic acid-modified copolymeric micelles could improve cellular uptake of curcumin in Hela and HepG2 cells compared with folic acid-unmodified micelles. In vitro cytotoxicity assay showed that folic acid-modified micelles improved anticancer activity against Hela and HepG2 cells in comparison to folic acidunmodified micelles. Meanwhile, both drug-loaded micelles demonstrated higher activity against Hela cell lines than HepG2.
Conclusion: The research results suggested that the folic acid-modified Y-shaped copolymeric micelles should be used to enhance hydrophobic anticancer drugs’ solubility and their specific delivery to folic acid receptors-overexpressed cancer.

 

HIGHLIGHTED ARTICLE – Vesicular Systems Containing Curcumin And Their Applications In Respiratory Disorders – Pharmaceutical Nanotechnology

PN-Articles_5-4-Dinesh Kumar Chellappan

To access the article, please visit: http://www.eurekaselect.com/154749

Free to download, Open Access Plus article from the journal ‘Letters in Drug Design & Discovery’

The article entitled Anaerobic Municipal Wastewater Treatment: A Beneficial Option for Developing Countries‘ in the journal Letters in Drug Design & Discovery, 2015, 12, 131-139 is now open for all to view and access.
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A small collection of eugenol- and curcumin-analog hydroxylated biphenyls was prepared by straightforward methods starting from natural 4-substituted-2-methoxyphenols and their antitumoral activity was evaluated in vitro. Two curcumin-biphenyl derivatives showed interesting growth inhibitory activities on different malignant melanoma cell lines with IC50 ranging from 13 to 1 µM. Preliminary molecular modeling studies were carried out to evaluate conformations and dihedral angles suitable for antiproliferative activity in hydroxylated biphenyls bearing a side aliphatic chain. 

Article: http://www.eurekaselect.com/124630/article
Journal: http://benthamscience.com/journal/abstracts.php?journalID=lddd&articleID=124630

Articles in New Thematic Issues of Anti-Cancer Agents in Medicinal Chemistry – 1

Novel Mechanisms of Anticancer Activities of Green Tea Component Epigallocatechin- 3-Gallate

Author(s): Le Zhang, Yaqing Wei and Jinsong Zhang

Affiliation: Key Laboratory of Tea Biochemistry and Biotechnology, Anhui Agricultural University of China, 130 West Changjiang Rd., Hefei 230036, Anhui, PR China.

Abstract

After water, tea is the most widely consumed beverage. The major active constituents in green tea are catechins, of which epigallocatechin-3-gallate (EGCG) is the most abundant and active compound. Animal experimental studies using EGCG alone or green tea catechins with EGCG being a major component have generated a mounting body of evidence suggesting that EGCG as a naturally occurring compound and commonly consumed beverage ingredient is a promising cancer preventive agent. However, the relationship between green tea consumption and reduced cancer risk seen from epidemiologic studies is not as encouraging as that observed in animal studies and remains inconclusive. In the present article, the achievements using EGCG or green tea catechins for cancer prevention were reviewed, the latest identified anticancer mechanisms of EGCG and the emerging mechanism-based cancer therapies of EGCG were outlined, and the potential reasons for the discrepancy in animal studies and epidemiological studies were tentatively analysed. On the basis of these analyses, it could be anticipated that future intervention trials in humans would be able to achieve consistent cancer prevention effects provided that the timely intervention of EGCG or green tea catechins at appropriate high-dose levels presumably approaching their upper safety limits have had been fully considered.
 
 

Curcumin: A Promising Agent Targeting Cancer Stem Cells

Author(s): Shufei Zang, Tao Liu, Junping Shi and Liang Qiao

Affiliation: The Affiliated Hospital of Hangzhou Normal University, NO.126, WenzhouRoad, Hangzhou 310015, Zhejiang Province, China.

Abstract

Cancer stem cells are a subset of cells that are responsible for cancer initiation and relapse. They are generally resistant to the current anticancer agents. Successful anticancer therapy must consist of approaches that can target not only the differentiated cancer cells, but also cancer stem cells. Emerging evidence suggested that the dietary agent curcumin exerted its anti-cancer activities via targeting cancer stem cells of various origins such as those of colorectal cancer, pancreatic cancer, breast cancer, brain cancer, and head and neck cancer. In order to enhance the therapeutic potential of curcumin, this agent has been modified or used in combination with other agents in the experimental therapy for many cancers. In this mini-review, we discussed the effect of curcumin and its derivatives in eliminating cancer stem cells and the possible underlying mechanisms.

 
 

Garlic-Derived Allyl Sulfides in Cancer Therapy

Author(s): Hai-Xia Cao, Ke-Xiang Zhu, Jian-Gao Fan and Liang Qiao

Affiliation: Department of Gastroenterology, Xinhua Hospital, Shanghai Jiaotong University School of medicine, Shanghai Key Laboratory of Pediatric Gastroenterology and Nutrition, Shanghai 200092, China.

Abstract

Garlic (Allium sativam L.) is widely used in traditional herbal remedies and alternative medicine. The potential health benefits of garlic are largely attributed to its metabolic byproducts. Extensive in vivo and in vitro studies has demonstrated that the garlic derivatives possess anti-cancer effects, but the underlying mechanisms are not completely understood. In this mini-review, we aim to summarize the reported biological effects of garlic products as anti-tumor agents, and present the possible molecular mechanisms responsible for the anti-carcinogenesis effects of garlic and its derivatives.

 
 

Part 1

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