Showing 4 results for Polymersome
H. Danafar, A. R. Nomani, M. Sadeghizadeh,
Volume 10, Issue 3 (9-2019)
Abstract
Nanotechnology is currently one of the promising approaches for cancer diagnosis and treatment. Among different materials that so far have been used for drug delivery, the systems based on the polymers are more attractive, due to their simple manufacturing processes and diversity in polymer functionalization and modification methods. Polyethyleneglycol (PEG) and polycaprolactone (PCL) are two FDA approved and biocompatible synthetic polymers which frequently have been used in the pharmaceutical industry. Apart from the delivery carriers, the active ingredient’s safety is also very challenging in case of cancer therapeutics. The chemotherapy agent’s side effects are one of the main patients’ death in many cancers. The naturally extracted curcumin is one of the most interesting anti-cancer agents with a proven selective effect on the cancerous cells which results in minimum side effects during the treatment. Curcumin has been tested as the main agent or in combination therapy of various cancers. Numerous studies have shown the safety and efficacy of curcumin at different administered doses. However, the main obstacle in the application of curcumin is its low aqueous solubility and low and variable bioavailability after administration. For that, in this study, we tried to enhance the solubility of curcumin using a novel diblock copolymer of PEG-PCL nanoparticulate system. At first, the PEG-PCL copolymer was synthesized and then characterized by GPC, FTIR, and H NMR methods. After that, curcumin was loaded in the micellar structure of PEG-PCL at an optimized encapsulation approach and then the toxicity of the prepared nanoparticles was assessed in MCF-7 cell culture. The results showed that the prepared nanoparticles could efficiently entrap the hydrophobic molecules of curcumin, improve its solubility and increase in vitro activity against cancer cell line.
Parvaneh Peyvand, Zahra Vaezi, Hossein Naderi-Manesh,
Volume 16, Issue 1 (12-2024)
Abstract
Hepatocellular carcinoma, predominant form of liver cancer, is the main cause of death in patients with liver cirrhosis. Podophyllotoxin, a natural anticancer compound, has ideal anti-tumor properties. However, its use is limited due to poor solubility and bioavailability. Finding a suitable drug delivery system have great importance in improving the bioavailability of podophyllotoxin. In this study, mPEG-PCL nanoparticles have been used for delivery of podophyllotoxin to liver cancer cells. mPEG-PCL copolymers were synthesized and characterized by DLS, FTIR and NMR analyses methods. The critical micellization concentration was 0.055 µg/ml. The z-average and surface charge of micelle was 186 ± 12 nm and -5.13 mV, respectively. podophyllotoxin was loaded in micelles in different w/w ratios of drug: copolymer. The size of the nanodrug was 214 ± 20 nm and the weight ratio of 1:1 with encapsulation efficiency of 77.36 ± 1.23 % was selected as the optimal ratio. The drug release results showed a significant difference between the rapid release of free podophyllotoxin and the more stable release of the loaded drug. At 37°C, drug release was higher, which was attributed to the destruction of polymersome structure at this temperature. According to the cytotoxicity study, the IC50 value for nanodrug (8.64 μg/ml) was lower than the IC50 value for the free drug (12.79 μg/ml), which showed the effect of improved cytotoxicity of nanodrug compared to the free drug. The results proved the polymersome can be potential carriers for delivery, controllable release and improve the toxicity effect of podophyllotoxin in cancer chemotherapy.
Volume 17, Issue 1 (4-2014)
Abstract
Objective: In recent decades, the anticancer effect of curcumin has been proven by several studies. Curcumin affects multiple cell signaling pathways and prevents cell proliferation, invasion, metastasis and angiogenesis. However, the aqueous solubility of curcumin and its bioavailability are very low which restricts its anticancer properties. In this research, we have synthesized a monomethoxy poly (ethylene glycol)-Oleate (mPEG-OA) di-block copolymer and used a surface PEGylated poly (amidoamine) (PAMAM) dendrimer to improve bioavailability of curcumin in cancer cells. Methods: Thecritical micelle concentration (CMC) of mPEG-OA, drug loading efficiencies, and cytotoxicity in the human glioblastoma cell line (U87MG) of all the prepared nanodevices were thoroughly investigated. Results: Atomic force microscopy (AFM) and dynamic light scattering (DLS) studies have shown that mPEG-OA have two common nanostructures, micelles and polymerosomes. mPEG-OA micelles had a very low CMC (0.03 g/l). The IC50 of free curcumin (0.01 methanol solution) was 48 μM, curcumin-loaded mPEG-OA was 24 μM , and curcumin-loaded PAMAM dendrimer was 13 μM. Moreover, the PEGylated PAMAM was non-cytotoxic. Conclusion: The results indicated that by using these nanocarriers, the bioavailability of curcumin significantly increased compared to free curcumin. Overall, this research revealed that these curcumin nanocarriers could be considered as appropriate drug delivery systems for curcumin delivery in cancer cells.
Volume 19, Issue 1 (5-2016)
Abstract
Objective: Numerous researches have been conducted to comprehend the anti-cancer effects of curcumin (Cu). Although the anti-proliferative properties of Cu on cancerous cells is known, the clinical application of this gold substrate is limited. This limitation is mostly due to low solubility, inefficient bioavailability, rapid metabolism, and improper uptake. In this study, we have synthesized a novel biodegradable gemini surfactant (Gs), after which the curcumin (Cu) molecules were encapsulated within the polymer to overcome its physicochemical limitations.
Methods: We prepared Gs-Cu nanoparticles by the nanoprecipitation method. Size and polydispersity index of the nanoparticles were determined by the dynamic light scattering (DLS) technique. The release profile of Cu from the polymer matrix was studied, and the MTT assay and cellular uptake of Gs-Cu on MDA-MB-231 cells were investigated in vitro.
Results: The Gs polymer had the capability to form polymersomes in an aqueous solution; a narrow size distribution was obtained (PDI≅0.3). The encapsulation efficiency approximated 87%. We observed a sustained release profile due to incorporation of Cu into the polymer matrix. The Gs-Cu complex showed more cytotoxicity compared to free Cu because of the higher rate of cellular internalization.
Conclusions: The data indicate that Gs polymersomes can be regarded as nanocarriers for hydrophobic curcumin molecules.
