pH-Responsive Hydrogel Beads Based on Alginate, κ-Carrageenan and Poloxamer for Enhanced Curcumin, Natural Bioactive Compound, Encapsulation and Controlled Release Efficiency (original) (raw)
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Bioorganic Chemistry, 2020
Curcumin, a molecule of immense pharmacological significance is also known to exhibit poor aqueous solubility and low bioavailability. Different strategies have been adopted to enhance the aqueous solubility of curcumin, but report on the effect of traditional excipients on curcumin solubility still stand in need of. Here, we presented the significance of different traditional excipients used in anti-inflammatory formulations on curcumin solubility. The endeavor has been undertaken with the hypothesis that "traditional formulation used since ages have a scientific basis". To meet the quest we encapsulated 28 different formulations containing varying concentrations of milk, sugar, cow milk fat, and black pepper in alginate hydrogels. After the characterization of formulations through FT-IR, solubility studies were conducted. Milk was found to be an essential component for improved curcumin availability. Individually, cow milk fat and piperine exhibited lesser effect but their synergistic effect was observed in the presence of milk. Dual behavior of sugar has been observed. Traditionally used excipients greatly enhanced the solubility of curcumin. The results have also been validated through anti-oxidant activities of different formulations. Intermolecular interactions have been explained using Molecular modeling studies.
Pharmaceutics
Curcumin comes from the plant species Curcuma longa and shows numerous pharmacological activities. There are numerous curcumin formulations with gels or cyclodextrins in order to increase its solubility and bioavailability. This paper presents the formulation of complex of curcumin with 2-hydroxypropyl-β-cyclodextrin in a thermosensitive hydrogel, based on N-isopropylmethacrylamide and N-isopropylacrylamide with ethylene glycol dimethacrylate as a crosslinker. The product was characterized by chemical methods and also by FTIR, HPLC, DSC, SEM, XRD. The results show that synthesis was successfully done. With an increase in the quantity of crosslinker in the hydrogels, the starting release and the release rate of curcumin from the formulation of the complex with hydrogels decreases. The release rate of curcumin from the gel complex formulation is constant over time. It is possible to design a formulation that will release curcumin for more than 60 days. In order to determine the mechan...
2018
Objective: Biohydrogel has gathered great interest in the pharmaceuticals field. This natural polymers were biodegradable, non-toxic, biocompatible, and its specific ability to response environment change can be considered for the controlled released matric of bioactive compound. In this study, the biohydrogel was synthesized by graft-copolymerization of acrylic acid onto carboxymethyl starch (CMS) and chitosan. The objective of this research was to determine the effect of CMS-chitosan ratio on the biohydrogel characteristic. Methods: The acrylic acid was grafted on to the backbone (3:1) by using cerric ammonium nitrate as the inisiator. A standarded curcumin was applied to test the binding potency of matrix. Results: A higher CMS ratio in the polymer mixture (4:1) revealed the highest swelling power (16.9 w/w) and percentage of curcumin absorption (17.34%). All the samples have the pH-responsive swelling properties, with the swelling trend was observed in the order of distilled wat...
Journal of Pharmaceutical Innovation, 2018
Purpose Curcumin (CUR), a natural polyphenolic compound, has several pharmacological uses, primarily regarding its antiinflammatory, chemotherapeutic, and antioxidant properties. However, to date, a significant drawback of curcumin is its poor bioavailability due to its low solubility and permeability. Therefore, the association of curcumin in polymeric nanocapsules may be an excellent strategy to increase its bioavailability. Methods Two nanocapsule systems were developed with an oily core of vitamin E surrounded by a biodegradable polymeric shell of either chitosan (NC-CS) or alginate (NC-ALG) capable of improving the encapsulation efficiency, stability, and permeability of CUR. NC-CS and NC-ALG showed particle sizes of approximately 116.7 ± 3.2 and 178 ± 7.9 nm, dispersities of 0.107 and 0.149, and zeta potentials of 24.4 ± 2.1 and − 49.0 ± 2.3 mV, respectively. Results The encapsulation efficiency was approximately 90% in both cases, and they were demonstrated to be stable under storage conditions for 3 months. Cytotoxicity studies performed in Caco-2 cells using the method of trypan blue dye revealed that even at a high concentration of chitosan and alginate (157.9 μg/cm 2 or 600 mg/mL), both of the nanocapsules were not toxic, exhibiting cell viability > 80%. The permeability was evaluated using Caco-2 cells as an in vitro model of the epithelial barrier. The obtained results show that the permeability of NC-CS and NC-ALG encapsulated CUR was considerably higher compared to that of an aqueous suspension. Conclusions The obtained results suggest that nanocapsules could improve the solubility, permeability, and stability of curcumin.
Polymeric Nanoparticles for Increasing Oral Bioavailability of Curcumin
Antioxidants, 2018
Despite the promising biological and antioxidant properties of curcumin, its medical applications are limited due to poor solubility in water and low bioavailability. Polymeric nanoparticles (NPs) adapted to oral delivery may overcome these drawbacks. Properties such as particle size, zeta potential, morphology and encapsulation efficiency were assessed. Then, the possibility of storing these NPs in a solid-state form obtained by freeze-drying, in vitro curcumin dissolution and cytocompatibility towards intestinal cells were evaluated. Curcumin-loaded Eudragit ® RLPO (ERL) NPs showed smaller particle diameters (245 ± 2 nm) and better redispersibility after freeze-drying than either poly(lactic-co-glycolic acid) (PLGA) or polycaprolactone (PCL) NPs. The former NPs showed lower curcumin encapsulation efficiency (62%) than either PLGA or PCL NPs (90% and 99%, respectively). Nevertheless, ERL NPs showed rapid curcumin release with 91 ± 5% released over 1 h. The three curcumin-loaded NPs proposed in this work were also compatible with intestinal cells. Overall, ERL NPs are the most promising vehicles for increasing the oral bioavailability of curcumin.
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.
Curcumin, a yellow polyphenol derived from the turmeric Curcuma longa, has been associated with a diverse therapeutic potential including anti-inflammatory, antioxidant, antiviral, and anticancer properties. However, the poor aqueous solubility and low bioavailability of curcumin have limited its potential when administrated orally. In this study, curcumin was encapsulated in a series of novel nano-microparticulate systems developed to improve its aqueous solubility and stability. The nano-microparticulate systems are based entirely on biocompatible, biodegradable, and edible polymers including chitosan, alginate, and carrageenan. The particles were synthesized via ionotropic gelation. Encapsulating the curcumin into the hydrogel nanoparticles yielded a homogenous curcumin dispersion in aqueous solution compared to the free form of curcumin. Also, the in vitro release profile showed up to 95% release of curcumin from the developed nano-microparticulate systems after 9 hours in PBS at pH 7.4 when freeze-dried particles were used.
Curcumin as a bioactive compound: biological properties and encapsulation methods
2020
Curcumin is a bioactive compound from turmeric which has different biological properties and health benefits such as antioxidant, anti-inflammatory, antimicrobial, and anticancer activities. However, the low solubility, poor bioavailability, and rapid degradation under neutral or alkaline pH conditions or when exposed to light, limit the food applications of curcumin. These problems can be solved by different strategies such as encapsulation. Therefore, different methods such as nanocomplexation, gelation, electro-spraying, complex coacervation, and pH-shifting approach have been applied to improve the solubility, stability, and bioavailability of curcumin. Consequently, the pharmacokinetic properties of curcumin including biological half-life and bioavailability/bio-accessibility can be improved resulting in better clinical and functional efficacy in vivo. Although the potentials of encapsulated forms of curcumin have been extensively studied in the literature, future studies can h...
BioMed Research International, 2013
Curcumin, a yellow polyphenol derived from the turmeric Curcuma longa, has been associated with a diverse therapeutic potential including anti-inflammatory, antioxidant, antiviral, and anticancer properties. However, the poor aqueous solubility and low bioavailability of curcumin have limited its potential when administrated orally. In this study, curcumin was encapsulated in a series of novel nano-microparticulate systems developed to improve its aqueous solubility and stability. The nano-microparticulate systems are based entirely on biocompatible, biodegradable, and edible polymers including chitosan, alginate, and carrageenan. The particles were synthesized via ionotropic gelation. Encapsulating the curcumin into the hydrogel nanoparticles yielded a homogenous curcumin dispersion in aqueous solution compared to the free form of curcumin. Also, the in vitro release profile showed up to 95% release of curcumin from the developed nano-microparticulate systems after 9 hours in PBS at pH 7.4 when freeze-dried particles were used.