Curcumin has been associated with the treatment of various diseases in traditional medicine, among them cancer. The major problems that prevent its approval as therapeutic agent are its low water solubility and its relatively low in vivo bioavailability. Liposomes are considered as effective drug carriers because of their ability to solubilize hydrophobic compounds and to alter their pharmacokinetic properties. The purpose of this study was the development of lyophilised liposomal curcumin fully characterized in terms of its physical properties [(zeta-potential, size, size distribution and Polydispercity index (PI)], and to evaluate its in vitro cytotoxic against colorectal cancer cell lines in a short-term and in a long-term (clonogenic) assay. Curcumin was incorporated in egg-phosphatidylcholine (EPC) liposomes at a drug to lipid molar ratio 1:14 achieving high incorporation efficiency close to 85%. The liposomal curcumin was lyophilized preserving thus its stability. The reconstitution of the formulation resulted in the original liposomal suspension. The release in FBS showed a plateau near 14% at 96 hours of incubation. The in vitro studies against colorectal cancer cell lines have shown that liposomes improve the activity of curcumin especially in the long-term assay and the liposomal formulation found to be more potent against HCT116 and HCT15, cell lines which express the MDR phenotype. EPC liposomal curcumin in a molar ratio of curcumin/EPC 1:14 has shown improved cytotoxic activity versus free curcumin against colorectal cancer cell lines. In vivo studies based on the recent findings are in progress in our laboratory.
"Dipeptide nanoparticle of curcumin inhibits tumor growth in mice . Phosphatidylcholine encapsulated curcumin exhibits antimalarial activity , inhibits vaginal inflammation  and induce cytotoxicity of cancer cells . There are several other cucrumin formulation are synthesized having more biological activities than curcumin. "
[Show abstract][Hide abstract] ABSTRACT: Curcumin (diferuloylmethane) is a yellow pigment present in the spice turmeric (Curcuma longa) that has been associated with antioxidant, anti-inflammatory, anticancer, antiviral, and antibacterial activities as indicated by over 6,000 citations. In addition, over one hundred clinical studies have been carried out with curcumin. One of the major problems with curcumin is perceived to be the bioavailability. How curcumin should be delivered in vivo, how bioavailable is it, how well curcumin is absorbed and how it is metabolized, is the focus of this review. Various formulations of curcumin that are currently available are also discussed.
Cancer Research and Treatment 01/2014; 46(1):2-18. DOI:10.4143/crt.2014.46.1.2 · 3.32 Impact Factor
"We have developed a nano-sized liposomal formulation with a narrow polydispersity, and achieved a high D/L mole ratio of 0.181 using EggPC liposomes. While a similar, high D/L, mole ratio for other lipophilic drugs such as paclitaxel (0.15),17 aryl-imidazole compound (ML220) (0.29),18 and curcumin (0.07)19 have been reported, the D/L mole ratio for other hydrophobic drugs such as ibuprofen (0.02)20 and cisplatin (0.05) were low.21 We previously achieved a maximum D/L mole ratio of 0.104 using DPPC liposomes, synthesized from a saturated lipid that maintained an IOP lowering effect for 50 days in the rabbit eyes.16 "
[Show abstract][Hide abstract] ABSTRACT: To report the development and therapeutic evaluation of a liposomal nanocarrier for sustained release of latanoprost, in the rabbit eye.
We fabricated latanoprost-loaded egg-phosphatidylcholine (EggPC) liposomes using the film hydration technique. The delivery vehicles were nano-sized (Z avg = 109 ± 18 nm), had a narrow poly dispersity index (PDI = 0.19 ± 0.04), and a very high loading efficiency (94% ± 5%). Based on in vitro data, we evaluated this formulation for lowering intraocular pressure (IOP) in rabbit eyes. Following a single subconjunctival injection of the latanoprost loaded formulation, the eyes were clinically monitored and the IOP recorded.
Latanoprost-loaded EggPC liposomes demonstrated a high drug/lipid mole ratio of 0.181, remained stable for at least 6 months on storage (4°C), and at least 1 month at 25°C. A slow and sustained release of 60% of latanoprost was achieved by 14 days in the in vitro release study. The same formulation demonstrated a greater sustained IOP lowering effect compared with daily administration of topical latanoprost beyond 90 days (4.8 ± 1.5 vs 2.5 ± 0.9 mmHg; P < 0.001). No signs of inflammation were evident in the eyes from slit-lamp examination analysis.
The loading required for a long-term sustained delivery of latanoprost for up to 90 days in the rabbit eyes was achieved with EggPC liposomes. A single injection of latanoprost-loaded EggPC liposomes can lower the IOP for up to 90 days, with a greater IOP lowering effect than daily topical administration of latanoprost.
International Journal of Nanomedicine 01/2012; 7:123-31. DOI:10.2147/IJN.S25468 · 4.38 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: In this work we developed a nanoformulation for anticancer saponin with chitosan for an enhanced and sustained release. The saponin loaded chitosan nanoparticles showed a particle size of 65±7nm. The synthesized nanoparticles were analyzed by FTIR, TG/DTA, SEM and AFM. The cytotoxicity of the nanoparticles was analyzed on L929, NIH-3T3, KB and PC3 which showed particles are non-toxic in a concentration range of 0.1–1.0mg/ml whereas the nanosaponin showed specific toxicity on PC3 and KB cell lines. The internalization of the nanosaponin on L929 and PC3 was confirmed by Rhodamine conjugation with the nanoparticles. Our preliminary studies support that nanosaponin could be an efficient therapeutic agent for cancer.
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