Molecular Inclusion Complex of Curcumin–β-Cyclodextrin Nanoparticle to Enhance Curcumin Skin Permeability from Hydrophilic Matrix Gel

Rachmawati, Heni; Edityaningrum, Citra Ariani; Mauludin, Rachmat

doi:10.1208/s12249-013-0023-5

Cited by 214 publications

(115 citation statements)

References 20 publications

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“…In our previous study, a similar drug release study was conducted for pure curcumin powder. The results showed that less than 15% of curcumin was released within 1 h. 39) By contrast, in this study, curcumin was completely released from the fiber within 1 h.…”

Section: Fig 7 Thermal Properties Of Materials In the Fibercontrasting

confidence: 80%

Intermolecular Interactions and the Release Pattern of Electrospun Curcumin-Polyvinyl(pyrrolidone) Fiber

Rahma

Munir

Khairurrijal

et al. 2016

Biological & Pharmaceutical Bulletin

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159

104

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An electrospun fiber of polyvinyl(pyrrolidone) (PVP)-Tween 20 (T20) with curcumin as the encapsulated drug has been developed. A study of intermolecular interactions was performed using Raman spectroscopy, Fourier transform infrared (FT-IR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD).The Raman and FT-IR studies showed that curcumin preferrably interacted with T20 and altered PVP chain packing, as supported by XRD and physical stability data. The hydroxyl stretching band in PVP shifted to a lower wavenumber with higher intenstity in the presence of curcumin and PVP, indicating that hydrogen bond formation is more intense in a curcumin or curcumin-T20 containing fiber. The thermal pattern of the fiber did not indicate phase separation. The conversion of curcumin into an amorphous state was confirmed by XRD analysis. An in vitro release study in phosphate buffer pH 6.8 showed that intermolecular interactions between each material influenced the drug release rate. However, low porosity was found to limit the hydrogen bond-mediated release.Key words curcumin; fiber; electrospinning; interaction; porosity; polymeric drug delivery system Curcumin is the major constituent of turmeric rhizome (Curcuma sp.).1) Curcumin has a number of demonstrated pharmacological effects, such as antioxidant, anti-inflammatory, anticancer, hepatoprotective, 1) antimicrobial, and antiviral. 2)Clinical trials have proven that curcumin is well tolerated by the body, with a maximum dose of 12 g daily.3) Unfortunately, the efficacy of curcumin is limited by its poor solubility in water, as well as its instability under light, heat, and alkaline conditions.1) The solubility of curcumin in aqueous buffer (pH 5) is reported to be 11 ng/mL.3) Moreover, the absorption of curcumin in the gastrointestinal tract is very low, leading to poor bioavailability (in animals and humans).2) Therefore, designing an effective delivery system is necessary in order to address the limitations of curcumin use. 1-3)A wide range of drug delivery systems has been developed to improve the bioavailability of poorly soluble drugs, including fast-dissolving tablets, 4) incorporation into a hydrophilic complex, 1) micellization, and solid dispersion. 5) Electrospinning, a technique of producing thin strands of fiber using high voltage, has opened up opportunities in the development of drug delivery systems. An optimized electrospinning process can produce nano-sized fibers. 6)The high surface area and porosity of these electrospun fibers are advantageous in their use as carriers for poorly water-soluble drugs.5) The high surface area generally increases the dissolution rate of the incorporated drug, thus potentially enhancing its bioavailability. 5)Therefore, the incorporation of curcumin into an electrospun fiber is expected to improve its oral bioavailability.Tailoring a suitable drug-loaded fiber requires careful selection of materials, in addition to an optimized production process and environment. Generally, the drug is mixed with a polymer s...

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Section: Fig 7 Thermal Properties Of Materials In the Fibercontrasting

confidence: 80%

Intermolecular Interactions and the Release Pattern of Electrospun Curcumin-Polyvinyl(pyrrolidone) Fiber

Rahma

Munir

Khairurrijal

et al. 2016

Biological & Pharmaceutical Bulletin

Self Cite

159

104

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“…Dia. : 21.5 mm) [29,30]. The drug is loaded films were suspended in glass vessels containing 50 ml of 0.1 M phosphate buffer saline (PBS; pH: 1.2., 4.5 and 7.4).…”

Section: Anti-oxidant Analysismentioning

confidence: 99%

“…The drug is loaded films were suspended in glass vessels containing 50 ml of 0.1 M phosphate buffer saline (PBS; pH: 1.2., 4.5 and 7.4). At appropriate time intervals (10,20,30,40, 60, 120 min) aliquots of solutions were withdrawn and the amount of curcumin released were evaluated by UV spectrophotometer at 424 nm [31]. The release was quantified by the following equation:…”

Section: Anti-oxidant Analysismentioning

confidence: 99%

Cur-Ca-Thione: A Novel Curcumin Concoction With Enhanced Water Solubility and Brain Bio-Availability

Shelat

Acharya

2016

Int J Pharm Pharm Sci

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Objective: Curcumin, is widely studied as a potential drug in treating various disorders but lacks applicability due to poor water solubility and tissue bioavailability. The main objective of the study was to develop a formulation of curcumin that has enhanced water solubility and brain bioavailability.Methods: A curcumin concoction was prepared using solvent evaporation technique taking casein and glutathione as vectors. Various process parameters were identified namely time, temperature, pH and vector while formulation parameters included drug entrapment, anti-oxidant activity, and water solubility. The concoctions were evaluated for in vitro release kinetics at three pH i.e. 1.2, 4.5 and 6.2 at six-time intervals i.e. 10, 20, 30, 40, 60, 120 min using dialysis bag membrane. The same kinetics was further validated using same time points with wistar rats and giving concoction at a single dose of 2 g/kg via the oral route.Results: A concoction i.e. CUR-CA-THIONE having significant entrapment efficiency (77.83%, 97.75%, 90.19%), water solubility (40, 350 and 45 times than normal curcumin) and DPPH activity (IC50 Conclusion:The experiment helps in concluding that CUR-CA-THIONE has improved its water solubility and is able to by-pass systemic circulation to targeted activity.: 28.91, 25.07 and 27.89) was evaluated in concoctions CUR-CA-THIONE-T.1, CUR-CA-THIONE-T.2 and CUR-CA-THIONE-T.3 respectively. These formulations were then carried out for in vitro release profile at different pH with average release obtained between 20-30 min. In vivo kinetics was studied by isolating tissues like brain, liver, lung, kidney and spleen in male wistar rats and maximum brain bioavailability was observed for CUR-CA-THIONE-T.3 at 30 min with 75 ng/g of brain tissue.

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“…Short-term clinical runs (6) demonstrated very low toxicity in a single daily doses of 12 and 8 g for 3 months. However, curcumin low solubility in aqueous solutions (7,8), instability in alkaline pH and short half-life lead to low oral bioavailability and therapeutic limitations (8)(9)(10)(11)(12)(13)(14)(15)(16). Curcumin solubility is a determining factor for its bioavailability when administered orally (17) and huge scientific work has been devoted to overcome this limitation (8,(18)(19)(20)(21)(22).…”

Section: Introductionmentioning

confidence: 99%

Microparticles Containing Curcumin Solid Dispersion: Stability, Bioavailability and Anti-Inflammatory Activity

et al. 2015

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Abstract. This work aimed at improving the solubility of curcumin by the preparation of spray-dried ternary solid dispersions containing Gelucire®50/13-Aerosil® and quantifying the resulting in vivo oral bioavailability and anti-inflammatory activity. The solid dispersion containing 40% of curcumin was characterised by calorimetry, infrared spectroscopy and X-ray powder diffraction. The solubility and dissolution rate of curcumin in aqueous HCl or phosphate buffer improved up to 3600-and 7.3-fold, respectively. Accelerated stability test demonstrated that the solid dispersion was stable for 9 months. The pharmacokinetic study showed a 5.5-fold increase in curcumin in rat blood plasma when compared to unprocessed curcumin. The solid dispersion also provided enhanced anti-inflammatory activity in rat paw oedema. Finally, the solid dispersion proposed here is a promising way to enhance curcumin bioavailability at an industrial pharmaceutical perspective, since its preparation applies the spray drying, which is an easy to scale up technique. The findings herein stimulate further in vivo evaluations and clinical tests as a cancer and Alzheimer chemoprevention agent.

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Molecular Inclusion Complex of Curcumin–β-Cyclodextrin Nanoparticle to Enhance Curcumin Skin Permeability from Hydrophilic Matrix Gel

Cited by 214 publications

References 20 publications

Intermolecular Interactions and the Release Pattern of Electrospun Curcumin-Polyvinyl(pyrrolidone) Fiber

Intermolecular Interactions and the Release Pattern of Electrospun Curcumin-Polyvinyl(pyrrolidone) Fiber

Cur-Ca-Thione: A Novel Curcumin Concoction With Enhanced Water Solubility and Brain Bio-Availability

Microparticles Containing Curcumin Solid Dispersion: Stability, Bioavailability and Anti-Inflammatory Activity

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