Effect of Cyclodextrin Complexation of Curcumin on its Solubility and Antiangiogenic and Anti-inflammatory Activity in Rat Colitis Model

Yadav, Vivek R.; Suresh, Sarasija; Devi, Kshama; Yadav, Seema

doi:10.1208/s12249-009-9264-8

Cited by 240 publications

(172 citation statements)

References 24 publications

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“…For example, structural modification or cyclodextrin complexation has been used as molecular strategies to enhance the oral bioavailability of curcumin. 35,36 Researchers have also investigated nanoscale formulations of curcumin, such as liposomes, microemulsions, and micelles, for potential therapeutic applications. [37][38][39][40][41][42] The nanoscale effect by which such drug delivery systems improve the oral performance of curcumin involves increasing the surface area and interactions of curcumin, thereby providing better water dispersibility to enhance its absorption.…”

Section: Resultsmentioning

confidence: 99%

Silica-coated flexible liposomes as a nanohybrid delivery system for enhanced oral bioavailability of curcumin

Li¹,

Zhang²,

Su³

et al. 2012

IJN

105

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Abstract:We investigated flexible liposomes as a potential oral drug delivery system. However, enhanced membrane fluidity and structural deformability may necessitate liposomal surface modification when facing the harsh environment of the gastrointestinal tract. In the present study, silica-coated flexible liposomes loaded with curcumin (CUR-SLs) having poor water solubility as a model drug were prepared by a thin-film method with homogenization, followed by the formation of a silica shell by the sol-gel process. We systematically investigated the physical properties, drug release behavior, pharmacodynamics, and bioavailability of CUR-SLs. CURSLs had a mean diameter of 157 nm and a polydispersity index of 0.14, while the apparent entrapment efficiency was 90.62%. Compared with curcumin-loaded flexible liposomes (CURFLs) without silica-coatings, CUR-SLs had significantly higher stability against artificial gastric fluid and showed more sustained drug release in artificial intestinal fluid as determined by in vitro release assays. The bioavailability of CUR-SLs and CUR-FLs was 7.76-and 2.35-fold higher, respectively, than that of curcumin suspensions. Silica coating markedly improved the stability of flexible liposomes, and CUR-SLs exhibited a 3.31-fold increase in bioavailability compared with CUR-FLs, indicating that silica-coated flexible liposomes may be employed as a potential carrier to deliver drugs with poor water solubility via the oral route with improved bioavailability.

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Section: Resultsmentioning

confidence: 99%

Silica-coated flexible liposomes as a nanohybrid delivery system for enhanced oral bioavailability of curcumin

Li¹,

Zhang²,

Su³

et al. 2012

IJN

105

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“…The CU-PC-C and CU-HSPC-C have lower protein binding, with no signs of hemolysis, demonstrating their suitability for therapeutic application. In vivo studies of CU complexes have shown improved bioavailability and therefore are more effective systems for delivering CU into tumors (Maiti et al, 2007;Yadav et al, 2009). Phospholipids, the major components of the complexes that have good biocompatibility, could promote the delivery through the cell membrane and enhance drug concentration in the cells, further enhancing the anti-cell effect of the drugs.…”

Section: Discussionmentioning

confidence: 99%

“…From the in vitro release study, it was evident that the release of CU from complexes was sustained and endured for a longer period of time as compared to plain CU (Figure 3). Release of CU was almost completed within 6 h, whereas it was evident that both complexes (CU-PC-C and CU-HSPC-C) exhibited faster dissolution rates (67.45% and 49.43%, respectively) up to 24 h. The enhancement of dissolution rate obtained with inclusion complexes could also be due to CU wettability and formation of readily soluble complexes in the dissolution medium (Yadav et al, 2009). …”

Section: In Vitro Dissolution Studymentioning

confidence: 98%

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Development, characterization and toxicological evaluations of phospholipids complexes of curcumin for effective drug delivery in cancer chemotherapy

et al. 2014

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The purpose of this study was to prepare and characterize the complexes between curcumin (CU) phosphatidylcholine (PC) and hydrogenated soya phosphatidylcholine (HSPC) and to evaluate their anticancer activity. These CU-PC and CU-HSPC complexes (CU-PC-C and CU-HSPC-C) were evaluated for various physical parameters like Fourier transform infrared spectroscopy, melting point, solubility, scanning electron microscopy and the in vitro drug release study. These data confirmed the formation of phospholipids complexes. The in vitro hemolysis study showed that the complex was non-hemolytic. The anti-cancer potential of the complexes was demonstrated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay in MCF-7 cell line. This increase may be due to the amphiphilic nature of the complexes, which significantly enhances the water and lipid solubility of the CU. Unlike the free CU (which showed a total of only 90% drug release at the end of 8 h), complex showed around 40-60% release at the end of 8 h in dissolution studies. It showed that (when given in equimolar doses) complexes have significantly decreased the amount of CU available for absorption as compared with CU-free drug. Both CU-PC-C and CU-HSPC-C were found to be non-toxic at the dose equivalent to 2000 mg/kg of body weight of CU in the toxicity study. Acute and subacute toxicity studies confirmed the oral safety of the formulation. A series of genotoxicity studies was conducted, which revealed the non-genotoxicity potential of the developed complexes. Thus, it can be concluded that the phospholipid complexes of CU may be a promising candidate in cancer therapy.

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“…However, around 2005, Razella Kurzrock's group at MD Anderson Cancer Center solubilized curcumin by encapsulating curcumin in liposomes, and successfully started demonstrating its high efficacy in suppressing the PAK1-dependent growth of human colon and pancreatic cancer xenografts in mice: Curcumin in liposomes (20-40 mg/kg) suppresses the growth of these cancers by 50% (35,36). Furthermore, in 2009 an Indian group led by Sarasija Suresh at Nootan Dental College in Bangalore found that a chemically synthesized beta-dextrin derivative called hydroxypropyl-beta-CD would be the best among CDs to solubilize curcumin effectively and showed both its antiangiogenic and anti-inflammatory effects in vivo (37). Thus, in the future (probably in a decade or so) curcumin in either liposomes or CDs would become available on the market for the therapy of these cancers and NF tumors as well.…”

Section: Curcumin (Turmeric)mentioning

confidence: 99%

Effective neurofibromatosis therapeutics blocking the oncogenic kinase PAK1

Miyata

2011

DD&T

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Neurofibromatosis (NF) is a family of genetic diseases which are caused by dysfunction of either NF1 gene or NF2 gene. One in 3,000 people suffer from this tumor-carrying NF. NF1 gene product is a RAS GTPase activating protein (GAP) of 2,818 amino acids, which normally attenuates the GTPdependent signal transducing activity of the G protein RAS. Dysfunction of this GAP leads to the abnormal activation of RAS, and eventually an oncogenic kinase called PAK1 as well. NF2 gene product is ''Merlin'' which directly inactivates PAK1. Thus, dysfunction of Merlin causes the abnormal activation of PAK1. In other words, dysfunction of NF1 gene (causing type 1 NF) is basically the same as dysfunction of NF2 gene (causing type 2 NF). In fact the growth of both NF1 and NF2 tumors requires PAK1, and all PAK1 blockers, synthetic chemicals or natural products, suppress the growth of these NF tumor cells both in vitro (cell culture) and in vivo (mice).However, until recently, no FDA-approved effective NF therapeutics is available on the market. Here a series of anti-PAK1 products shall be introduced, which would be potentially useful for the life-long treatment of NF patients in the future. These include the most potent HDAC (histone deacetylase) inhibitor FK228 (IC 50 : around 1 nM), that eventually blocks PAK1, the direct PAK1 inhibitor PF3758309 (IC 50 : around 10 nM), a CAPE (caffeic acid phenethyl ester)-based propolis extract called ''Bio 30'' from NZ (New Zealand), and an ARC (artepillin C)-based green propolis extract (GPE) from Brazil. Although the first two drugs are potent, none of them is available on the market as yet. The last two natural (bee-made) products are available on the market, and have been used for the therapy of NF and tuberous sclerosis (TSC) as well as many PAK1-dependent solid cancers such as breast and pancreatic cancers as well as glioma, which altogether represent more than 70% of all human cancers. Since PAK1 is not essential for the normal cell growth, propolis extracts cause no side effects.

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Effect of Cyclodextrin Complexation of Curcumin on its Solubility and Antiangiogenic and Anti-inflammatory Activity in Rat Colitis Model

Cited by 240 publications

References 24 publications

Silica-coated flexible liposomes as a nanohybrid delivery system for enhanced oral bioavailability of curcumin

Silica-coated flexible liposomes as a nanohybrid delivery system for enhanced oral bioavailability of curcumin

Development, characterization and toxicological evaluations of phospholipids complexes of curcumin for effective drug delivery in cancer chemotherapy

Effective neurofibromatosis therapeutics blocking the oncogenic kinase PAK1

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