Development of curcuminoids loaded poly(butyl) cyanoacrylate nanoparticles: Physicochemical characterization and stability study (original) (raw)
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NANoPARtIcLes As PLAtFoRMs FoR DeLIVeRY oF cURcUMIN
2015
Curcumin, the active polyphenol isolated from Curcuma Longa, exhibited potent pleiotropic, antineoplastic activity, attributed with minimal toxicity to normal cells. Unfortunately, the clinical implementation of curcumin is limited due to its instability in physiological pH, low aqueous solubility (11 ng/ml) associated with extremely low systemic bioavailability after oral administration of 8 g/day. An intriguing approach to overcome these limitations is incorporation of curcumin in nanoparticles as delivery platforms such as solid lipid nanoparticles, nanoemulsions, liposomes and macrocyclic cavitands. A promising strategy for improvement of unfavorable physicochemical characteristics of curcumin consisting of its simultaneous loading in the phospholipid bilayer membrane and in the aqueous cavity of liposomes as inclusion complex with macrocyclic cavitands is presented.
Curcumin, a polyphenol derived from turmeric has many health benefits such as anticancerous, antioxidant, antidepressant etc. But its clinical use as an anticancerous agent is limited by its poor aqueous solubility and poor bioavailability. To enhance its bioavailability, in the present study curcumin was encapsulated in the Poly(butylene succinate) (PBS) nanospheres as a carrier. The PBS polymer (PBS-0) and curcumin loaded PBS nano particles were synthesized and analysed for their structure, morphology, thermal stability, Zeta potential, Particle size and invitro curcumin release features. Average PBS nanoparticle size for pure PBS and curcumin loaded PBS were found to be 214 and 354 nm respectively. MTT assay of PBS revealed that it was biocompatible and curcumin loaded PBS nano particle showed inhibitory effect on the growth of MCF-7 cancer cell line. DSC Study indicated a possible PBS-Curcumin interaction. In-vitro release studies both with curcumin loaded PBS-0 and curcumin loaded PBS nanoparticle in phosphate buffer saline revealed that the release was very gradual and sluggish in the former and rapid and controlled in the latter. For example, unlike curcumin loaded PBS-0 which released only 2% of curcumin after 180minutes, the curcumin loaded PBS nanoparticle released 17% of the curcumin for the same duration.
Latin American Journal of Pharmacy, 2010
Polymeric and lipid nanocapsules suspensions of the natural compound curcumin were prepared in order to overcome limitations associated with its clinical applications, such as poor aqueous solubility and susceptibility to hydrolytic and photochemical degradation. Nanocapsule suspensions were prepared by nanoprecipitation and phase inversion methods, respectively. The curcumin formulations were investigated for physicochemical characteristics and in vitro drug release. The hydrolytic and photochemical degradation of the drug associated with the nanocarriers was also determined. For all formulations, the entrapment efficiency values were higher than 99 %. The aqueous colloidal suspensions of curcumin resulted in an increase in drug concentration by a factor of up to 46.103 times. Moreover, stability studies indicated that nanoencapsulation slows down the hydrolytic and photochemical degradations of curcumin. The strategy of nanoencapsulation into polymeric and lipid nanocapsules produced a formulation of curcumin with high drug loading and improved stability, representing a good strategy for the delivery of this drug.
Biochimica et Biophysica Acta (BBA) - General Subjects, 2014
Background: Hybrid materials are synthesized using hydrophilic polymer and lipids which ensure their long term systemic circulation through intravenous administration and enhance loading of hydrophobic drugs. The purpose of this study is to prepare, characterize and evaluate the in vitro efficacy of curcumin loaded polyhydroxyethyl methacrylate/stearic acid nanoparticles in MCF-7. Methods: C-PSA-NPs, prepared using the emulsification-solvent evaporation method were characterized by dynamic laser scattering, SEM, AFM, FT-IR, X-ray diffraction, and TGA. The in vitro release behavior was observed in PBS pH 7.4, the anticancer potential was analyzed by MTT assay, cell cycle and apoptosis studies were performed through flow cytometry. C-PSA-NPs drug localization and cancer cell morphological changes were analyzed in MCF-7 cell line. Results: C-PSA-NPs exhibited the mean particle size in the range of 184 nm with no aggregation. The surface charge of the material was around − 29.3 mV. Thermal studies (TGA) and surface chemistry studies (FT-IR, XRD) showed the existence of drug curcumin in C-PSA-NPs. The MTT assay indicated higher anticancer properties and flow cytometry studies revealed that there were better apoptotic activity and maximum localization of C-PSA-NPs than curcumin. Conclusions: Polymer lipid based drug delivery appeared as one of the advancements in drug delivery systems. Through the present study, a novel polymer lipid based nanocarrier delivery system loaded with curcumin was demonstrated as an effective and potential alternative method for tumor treatment in MCF-7 cell line.
Curcumin Delivery Mediated by Bio-Based Nanoparticles: A Review
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Todays, nano-pharmaceutics is emerging as an important field of science to develop and improve efficacy of different drugs. Although nutraceuticals are currently being utilized in the prevention and treatment of various chronic diseases such as cancers, a number of them have displayed issues associated with their solubility, bioavailability, and bio-degradability. In the present review, we focus on curcumin, an important and widely used polyphenol, with diverse pharmacological activities such as anti-inflammatory, anti-carcinogenic, anti-viral, etc. Notwithstanding, it also exhibits poor solubility and bioavailability that may compromise its clinical application to a great extent. Therefore, the manipulation and encapsulation of curcumin into a nanocarrier formulation can overcome these major drawbacks and potentially may lead to a far superior therapeutic efficacy. Among different types of nanocarriers, biological and biopolymer carriers have attracted a significant attention due t...
Curcumin Polymer Based Nanospheres: Encapsulation and In Vitro Release
2020
Curcumin is a yellow pigmented polyphenol, having multiple medicinal uses due to its anti-inflammatory, antioxidant and antimicrobial effects. The most important effect is its potential use in chemothearpy for cancer treatment. In this study curcumin is encapsulated in Poly(DL-lactide-co-glycolide) nanospheres using solvent evaporation technique by means of Tween 80 and Span 80 as surfactants. Drug encapsulation, drug loading, particle size, morphology, FT-IR analysis and in-vitro studies, were conducted to characterize the formulated nanospheres.The spherical nanoshperes showed a size ranging between 60 and 130 nm, having a maximum drug encapsulation of 24%. The lack of interaction between both drug and polymer during the nanosphere formulation was proven during the FT-IR study. The in-vitro studies showed a fast drug release.
Polymers
Polymeric lipid hybrid nanoparticles (PLHNs) are the new generation of drug delivery systems that has emerged as a combination of a polymeric core and lipid shell. We designed and optimized a simple method for the preparation of Pluronic F-127-based PLHNs able to load separately demethoxycurcumin (DMC) and bisdemethoycurcumin (BDM). CUR was used as a model compound due to its greater availability from turmeric and its structure similarity with DMC and BDM. The developed method produced DMC and BDM-loaded PLHNs with a size average of 75.55 ± 0.51 and 15.13 ± 0.014 nm for DMC and BDM, respectively. An FT-IR analysis confirmed the encapsulation and TEM images showed their spherical shape. Both formulations achieved an encapsulation efficiency ≥ 92% and an exhibited significantly increased release from the PLHN compared with free compounds in water. The antioxidant activity was enhanced as well, in agreement with the improvement in water dissolution; obtaining IC50 values of 12.74 ± 0.0...
Design and characterization of nanoparticles as platforms for delivery of curcumin
2015
Curcumin, the yellow powder derived from the plant Curcuma Longa, exhibited numerous therapeutic applications against wide range of chronic diseases such as diabetes, pancreatitis, arthritis, neurodegenerative diseases and various types of cancer. The mechanism of antineoplastic activity of curcumin is through modulation of cell signaling pathways, mainly blockage of nuclear factor kappa B (NF-κB) activation and induction of apoptosis in different types of human cancer cell lines, associated with excellent safety profile. Despite the numerous advantages, the clinical realization of curcumin potential is limited because of its extremely low aqueous solubility and bioavailability after oral administration. An intriguing strategy to overcome these limitations is the design of nanosized vehicles for efficient delivery of curcumin. The present contribution is focused on newly-synthetized PEGylated tert-butylcalix[4]arene, used for preparation of various platforms for delivery of curcumin...
Curcumin-hybrid Nanoparticles in Drug Delivery System
Asian Journal of Nanoscience and Materials, 2019
Extensive studies on curcumin have improved that it has certain therapeutic impact for different kinds of diseases such as cancer. Regardless of its positive features, its application is hampered by its low water solubility, bioavailability, and low cellular uptake. During recent years, several ways have been developed to protect curcumin from degradation and increase the capacity of targeting unhealthy cells. The progress in nanotechnology encouraged nanotechnologists to formulate nanoparticles encapsulating curcumin, such as polymer nanoparticles, solid nanoparticles, liposome/lipid nanoparticles, micelles, dendrimers, polymer conjugates, etc. to enhance sustained release of curcumin at target cells and to improve curcumin bioavailability. Nowadays, newer formulations of nanoparticles as called Hybrid nanoparticles are designed in order to achieve efficient and specific curcumin targeted compound that result in the improved therapeutic efficacy of curcumin with high biocompatibility associated with aptamers, folic acid, chitosan coated halloysite loaded with curcumin-Au hybrid nanoparticle etc. This review describes a number of formulated hybrid nanoparticles and their efficacy in specific targeting to cancerous cells.
Delivery carrier of curcumin based on nanotechnology : A review
IOP Conference Series: Earth and Environmental Science, 2019
Curcumin is a polyphenolic compound derived from the rhizome of turmeric. It has been widely used as a medicine, condiment and food additives. Curcumin has several biological activities such as anti-oxidation, anti-inflammatory, liver protection, anti-tumor, anti-atherosclerosis, inhibition of obesity, anti-aging, neuroprotection, and anti-senile dementia, it has been applied in functional food in recent years. In view of the current shortcomings of curcumin, such as poor water solubility, instability, and low bioavailability, improving its bioavailability will be the main research direction in the future. This paper mainly discussed the source and physicochemical properties of curcumin, as well as the research progress of delivery carrier of curcumin including nanoparticles of protein matrix, nanoparticles of polysaccharide matrix and nanoparticles of protein polysaccharide composite matrix. Besides, it discussed the application of nanoparticles in improving the solubility, stabili...