Effect of HPβCD on solubility and transdermal delivery of capsaicin through rat skin

Zi, Peng; Yang, Xinghao; Kuang, Huifen; Yang, Yu−Ching; Yu, Lili

doi:10.1016/j.ijpharm.2008.03.001

Cited by 39 publications

(28 citation statements)

References 26 publications

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“…Thermal behaviors of CAP, MPEG-PCL, NPs, blank NPs and the physical mixture of CAP and the synthesized copolymer were analyzed by DSC and the results of thermal analysis are shown in Figure 4. CAP exhibits a melting peak between 63 °C and 70 °C, centered at approximately 67 °C as observed in the figure, which was consistent with a previous report [25] . MPEG-PCL showed a melting point at approximately 61 °C as well.…”

Section: Wwwnaturecom/aps Peng W Et Alsupporting

confidence: 92%

Oral delivery of capsaicin using MPEG-PCL nanoparticles

et al. 2014

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Aim: To prepare a biodegradable polymeric carrier for oral delivery of a water-insoluble drug capsaicin (CAP) and evaluate its quality. Methods: CAP-loaded methoxy poly (ethylene glycol)-poly(ε-caprolactone) nanoparticles (CAP/NPs) were prepared using a modified emulsification solvent diffusion technique. The quality of CAP/NPs were evaluated using transmission electron microscopy, powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared techniques. A dialysis method was used to analyze the in vitro release profile of CAP from the CAP/NPs. Adult male rats were orally administered CAP/NPs (35 mg/kg), and the plasma concentrations of CAP were measured with a validated HPLC method. The morphology of rat gastric mucosa was studied with HE staining. Results: CAP/NPs had an average diameter of 82.54±0.51 nm, high drug-loading capacity of 14.0%±0.13% and high stability. CAP/NPs showed a biphasic release profile in vitro: the burst release was less than 25% of the loaded drug within 12 h followed by a more sustained release for 60 h. The pharmacokinetics study showed that the mean maximum plasma concentration was observed 4 h after oral administered of CAP/NPs, and approximately 90 ng/mL of CAP was detected in serum after 36 h. The area under the curve for the CAP/NPs group was approximately 6-fold higher than that for raw CAP suspension. Histological studies showed that CAP/NPs markedly reduced CAP-caused gastric mucosa irritation. Conclusion: CAP/NPs significantly enhance the bioavailability of CAP and markedly reduce gastric mucosa irritation in rats.

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Section: Wwwnaturecom/aps Peng W Et Alsupporting

confidence: 92%

Oral delivery of capsaicin using MPEG-PCL nanoparticles

et al. 2014

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“…Capsaicin, a highly hydrophobic molecule, is conventionally administered topically in the form of ointments and gels. Most of these formulations employ organic solvents or surfactants, such as ethanol, propylene glycol and sodium lauryl sulfate as the solubilizers for capsaicin, which often disturbed or interacted with the intercellular lipids or keratin of human skin [11]. It was also reported that the increased concentrations of ethanol and isopropanol in the topical formulations reduce the percutaneous effect of capsaicin [12].…”

Section: Methodsmentioning

confidence: 99%

“…Nanoencapsulated capsaicin prepared by the simple coacervation method, achieved improved bioavailability as well as covering the pungent odor usually associated with capsaicin formulations [14]. Hydroxypropyl-β-cyclodextrin complex was prepared as a mean to increase its transdermal delivery [11]. Several other novel drug delivery systems for capsaicin such as niosomes, microemulsions, lipid-polymer hybrid nanoparticles have also been developed [15,16].…”

Section: Methodsmentioning

confidence: 99%

Topical Delivery System for Phytochemicals: Capsaicin and Capsicum Tincture

Thapa¹,

Pepić²,

Vanić³

et al. 2014

Journal of Pharmaceutics and Drug Development

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Annex Publishers | www.annexpublishers.com Capsaicin, an active ingredient of Capsicum fruit, is currently undergoing "revival" in the clinical management of pain. However, the choice of its formulation is rather limited to the use of "old-fashioned" tinctures and recently the patches. In an attempt to improve the therapeutic outcome and develop its skin-friendly formulation, we prepared the vesicle-based drug delivery system with capsaicin. Moreover, the use of standardized Capsicum extract, rather than a single active ingredient, is proposed to lead to simplified and more cost-effective formulations. Phospholipid-based vesicles, namely liposomes and ethosomes, were prepared with capsaicin, Capsicum tincture or Capsicum powder and characterized for particle size, entrapment efficiency and stability. The vesicular dispersions were incorporated in the hydrogels to increase the formulation stability, its retention time at the skin and overall acceptability. Both the standardized crude Capsicum powder and Capsicum tincture were successfully employed as sources of capsaicin which is, to the best of our knowledge, reported for the first time. The reported phospholipid-based delivery system for capsaicin could represent an improved topical treatment of arthritic pain.

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“…First, CDs can form hydrophilic inclusion complexes with lipophilic compounds in aqueous solution to improve drug solubility without changing their intrinsic ability to permeate the lipophilic barrier (Zi et al, 2008). During the complex formation, no covalent bonds are formed or broken, and in the aqueous solution the complexes are readily dissociated to release the free drug (Loftsson et al, 1998).…”

Section: Cyclodextrinsmentioning

confidence: 99%

“…During the complex formation, no covalent bonds are formed or broken, and in the aqueous solution the complexes are readily dissociated to release the free drug (Loftsson et al, 1998). Up to date, most of CD and its derivatives have demonstrated their potential as solubilizers to promote percutaneous absorption of many different drugs (Loftsson et al, 1995;Ventura et al, 2006;Zi et al, 2008). In addition, it was indicated that the solubility enhancing effect was closely depended on the concentration of CDs applied in the donor vehicle.…”

Section: Cyclodextrinsmentioning

confidence: 99%

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

2013

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The highly organized structure of the stratum corneum provides an effective barrier to the drug delivery into or across the skin. To overcome this barrier function, penetration enhancers are always used in the transdermal and dermal drug delivery systems. However, the conventional chemical enhancers are often limited by their inability to delivery large and hydrophilic molecules, and few to date have been routinely incorporated into the transdermal formulations due to their incompatibility and local irritation issues. Therefore, there has been a search for the compounds that exhibit broad enhancing activity for more drugs without producing much irritation. More recently, the use of biomaterials has emerged as a novel method to increase the skin permeability. In this paper, we present an overview of the investigations on the feasibility and application of biomaterials as penetration enhancers for transdermal or dermal drug delivery systems.

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Effect of HPβCD on solubility and transdermal delivery of capsaicin through rat skin

Cited by 39 publications

References 26 publications

Oral delivery of capsaicin using MPEG-PCL nanoparticles

Oral delivery of capsaicin using MPEG-PCL nanoparticles

Topical Delivery System for Phytochemicals: Capsaicin and Capsicum Tincture

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

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