Transdermal permeation of drugs with differing lipophilicity: Effect of penetration enhancer camphor

Xie, Feng; Chai, Jia-ke; Hu, Quan; Yu, Yang; Ma, Li; Liu, Lingying; Zhang, Xu-long; Li, Bailing; Zhang, Donghai

doi:10.1016/j.ijpharm.2016.05.004

Cited by 54 publications

(43 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Drug delivery across the skin remains as an important challenge in the development of drug delivery systems. This is mainly attributed to the highly organized intercellular lipids and poor permeability of stratum corneum [ 26 ]. It is also well-known that lipophilic molecules move across the barrier by a transcellular mechanism whereas hydrophilic agents are likely to follow a paracellular pathway to cross the skin.…”

Section: Discussionmentioning

confidence: 99%

Fucoxanthin-Containing Cream Prevents Epidermal Hyperplasia and UVB-Induced Skin Erythema in Mice

et al. 2018

View full text Add to dashboard Cite

Microalgae represent a source of bio-active compounds such as carotenoids with potent anti-inflammatory and antioxidant properties. We aimed to investigate the effects of fucoxanthin (FX) in both in vitro and in vivo skin models. Firstly, its anti-inflammatory activity was evaluated in LPS-stimulated THP-1 macrophages and TNF-α-stimulated HaCaT keratinocytes, and its antioxidant activity in UVB-irradiated HaCaT cells. Next, in vitro and ex vivo permeation studies were developed to determine the most suitable formulation for in vivo FX topical application. Then, we evaluated the effects of a FX-containing cream on TPA-induced epidermal hyperplasia in mice, as well as on UVB-induced acute erythema in hairless mice. Our results confirmed the in vitro reduction of TNF-α, IL-6, ROS and LDH production. Since the permeation results showed that cream was the most favourable vehicle, FX-cream was elaborated. This formulation effectively ameliorated TPA-induced hyperplasia, by reducing skin edema, epidermal thickness, MPO activity and COX-2 expression. Moreover, FX-cream reduced UVB-induced erythema through down-regulation of COX-2 and iNOS as well as up-regulation of HO-1 protein via Nrf-2 pathway. In conclusion, FX, administered in a topical formulation, could be a novel natural adjuvant for preventing exacerbations associated with skin inflammatory pathologies as well as protecting skin against UV radiation.

show abstract

Section: Discussionmentioning

confidence: 99%

Fucoxanthin-Containing Cream Prevents Epidermal Hyperplasia and UVB-Induced Skin Erythema in Mice

et al. 2018

View full text Add to dashboard Cite

show abstract

“…The frequencies of these amide bonds shifts to lower or higher frequencies due to change in protein conformation [29] and from the spectra (Fig. 6) it was seen that the frequency of the amide band of the test shifted toward the higher frequency in comparison to the control which helps us to conclude that the essential oil under investigation (patchouli oil) enhances the permeation by possible disruption of stratum corneum lipids and also by changing protein conformations.…”

Section: Das and Ahmedmentioning

confidence: 72%

“…It also showed 2 amide vibrations within the range of 1500~1700 cm ), which were one of the important parameters to investigate the alteration in the structure of the lipids and keratin present in stratum corneum induced by penetration enhancers [29]. The frequencies of these amide bonds shifts to lower or higher frequencies due to change in protein conformation [29] and from the spectra (Fig.…”

Section: Das and Ahmedmentioning

confidence: 94%

Formulation and Evaluation of Transdermal Patch of Indomethacin Containing Patchouli Oil as Natural Penetration Enhancer

Das¹,

Ahmed²

2017

Asian J Pharm Clin Res

View full text Add to dashboard Cite

Objective: To develop a transdermal patch of Indomethacin using patchouli oil as a natural enhancer to increase transdermal permeation of the drug from the matrix system across rat epidermis. Materials and Methods:The chemical characterization of patchouli oil was done by gas chromatography-mass spectrometry. Transdermal patches of indomethacin were formulated after studying the drug-excipient compatibility studies by differential scanning calorimetry and Fourier transform infrared spectroscopy (FTIR). The transdermal patches were evaluated for various physiochemical properties. In-vitro transdermal permeation was carried using modified Keshary-Chein diffusion cell across rat epidermis. FTIR studies of rat epidermis were done to understand the mechanism of the permeation enhancing effect of the oil from the matrix patch. Result:The results of physiochemical parameters of the transdermal patch were found satisfactory. The transdermal flux obtained of the different concentration of patchouli oil tend to increase with increasing concentration of the oil and the maximum transdermal flux of 61.92 ± 0.89 µg/cm 2 /hr was obtained with formulation F7 (containing 1% w/v of patchouli oil) which is similar to the flux of the formulation F2 containing standard enhancer dimethyl sulphoxide. The skin irritation test did not show any edema and the FTIR data of rat epidermis indicated that patchouli oil enhances transdermal permeation of indomethacin by partial extraction of lipids in the stratum corneum. Conclusion:Thus, the results showed a potential enhancing effect of patchouli oil on the transdermal permeation of the model drug indomethacin and may be used as natural permeation enhancer in transdermal drug delivery systems.

show abstract

“…Penetration enhancers are used with the aim to improve the transdermal drug delivery [ 35 ]. Several chemicals such as sulphoxides, azones, pyrrolidones, alcohols, glycols, surfactants, fatty acids, essential oils, and terpenes have been proposed for their ability to reversibly decrease the barrier resistance, allowing drug penetration into the skin at a greater rate [ 36 , 37 ]. As a result, penetration enhancers represent an alternative to improve the permeability and, consequently, the duration of drug action.…”

Section: Introductionmentioning

confidence: 99%

Human Skin Permeation Studies with PPARγ Agonist to Improve Its Permeability and Efficacy in Inflammatory Processes

Silva-Abreu

Espinoza

Rodríguez-Lagunas

et al. 2017

IJMS

View full text Add to dashboard Cite

Rosacea is the most common inflammatory skin disease. It is characterized by erythema, inflammatory papules and pustules, visible blood vessels, and telangiectasia. The current treatment has limitations and unsatisfactory results. Pioglitazone (PGZ) is an agonist of peroxisome proliferator-activated receptors (PPARs), a nuclear receptor that regulates important cellular functions, including inflammatory responses. The purpose of this study was to evaluate the permeation of PGZ with a selection of penetration enhancers and to analyze its effectiveness for treating rosacea. The high-performance liquid chromatography (HPLC) method was validated for the quantitative determination of PGZ. Ex vivo permeation experiments were realized in Franz diffusion cells using human skin, in which PGZ with different penetration enhancers were assayed. The results showed that the limonene was the most effective penetration enhancer that promotes the permeation of PGZ through the skin. The cytotoxicity studies and the Draize test detected cell viability and the absence of skin irritation, respectively. The determination of the skin color using a skin colorimetric probe and the results of histopathological studies confirmed the ability of PGZ-limonene to reduce erythema and vasodilation. This study suggests new pharmacological indications of PGZ and its possible application in the treatment of skin diseases, namely rosacea.

show abstract

Transdermal permeation of drugs with differing lipophilicity: Effect of penetration enhancer camphor

Cited by 54 publications

References 29 publications

Fucoxanthin-Containing Cream Prevents Epidermal Hyperplasia and UVB-Induced Skin Erythema in Mice

Fucoxanthin-Containing Cream Prevents Epidermal Hyperplasia and UVB-Induced Skin Erythema in Mice

Formulation and Evaluation of Transdermal Patch of Indomethacin Containing Patchouli Oil as Natural Penetration Enhancer

Human Skin Permeation Studies with PPARγ Agonist to Improve Its Permeability and Efficacy in Inflammatory Processes

Contact Info

Product

Resources

About