Transfollicular drug delivery—Is it a reality?

Meidan, Victor M.; Bonner, Michael; Michniak, B. B.

doi:10.1016/j.ijpharm.2005.09.025

Cited by 139 publications

(93 citation statements)

References 66 publications

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“…While the follicular opening constitute only about 0.1% of the total skin area (Meidan et al, 2005), the hair follicle represents an invagination of the epidermis extending deep into the dermis and thus provides a greater actual area for potential absorption (Agarwal et al, 2000;Singh et al, 2000).…”

Section: Introductionmentioning

confidence: 99%

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Noninvasive and persistent transfollicular drug delivery system using a combination of liposomes and iontophoresis

Kajimoto

Yamamoto

Watanabe

et al. 2011

International Journal of Pharmaceutics

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Iontophoresis is a promising technique for enhancing transdermal administration of charged drugs. However, conventional iontophoresis is not sufficient for effective delivery of large, hydrophilic, or electrically neutral molecules. In this study, we utilized charged liposomes as carriers, focused on a transfollicular route for delivery of the liposomes, and optimized iontophoretic conditions and lipid composition for this method in both in vitro and in vivo conditions.As a result, we identified the optimum condition (lipid composition:DOTAP/EPC/Chol=2:2:1, current supply: 0.45 mA/cm 2 , duration: 1 hr) for effective iontophoretic delivery of aqueous solution, which can not be transferred into the skin without charged liposomes. We also examined the pharmacological effects of iontophoresis of liposomes encapsulating insulin (INS-lipo) using a rat model of type I diabetes. Interestingly, iontophoresis of INS-lipo onto a diabetes rat skin resulted in a gradual decrease in blood glucose levels, with levels reaching 20% of initial values at 18 hr after administration. These lower blood glucose levels were maintained for up to 24 hr. Significant amount of insulin were also detected in plasma 18 hr after iontophoresis of INS-lipo. We succeeded in developing a non-invasive and persistent transfollicular drug delivery system that used a combination of liposomes and iontophoresis.

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Section: Introductionmentioning

confidence: 99%

“…In addition, there is an extensive capillary network associated with the upper dermal vasculature (Meidan et al, 2005). According to these features, the hair follicle might have great potential for drug delivery into the viable skin layers or the systemic circulation.…”

Section: Introductionmentioning

confidence: 99%

Noninvasive and persistent transfollicular drug delivery system using a combination of liposomes and iontophoresis

Kajimoto

Yamamoto

Watanabe

et al. 2011

International Journal of Pharmaceutics

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“…15 Each skin sample had a hair follicle density on average between 30 and 40 follicles per application area (1.96 cm 2 ). One microdrop of nail varnish using a blunt 27-gauge needle was carefully placed beside each hair follicle orifice and dried for 5 minutes to completely block the follicular shunt.…”

Section: Selectively Blocked Hair Folliclementioning

confidence: 99%

“…It can be remained in the lipid portion of the stratum corneum, and can fluidize or perturb the integrity of the barrier function of the stratum corneum for enhanced transport of both hydrophilic and hydrophobic drugs through the skin. 15 Polyethylene glycol (PEG), a hydrophilic polymer, grafted onto the surface of the liposomes (PEGylated liposomes, PL), was reported to enhance skin penetration of zidovudine by binding to water molecules, increasing the hydration of the stratum corneum. 16 In addition, our previous work reported that d-limonene containing PL provided a synergistic effect to enhance penetration of hydrophilic compounds into and through the skin.…”

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confidence: 99%

Mechanistic study of decreased skin penetration using a combination of sonophoresis with sodium fluorescein-loaded PEGylated liposomes with D-limonene

Rangsimawong

Opanasopit

Rojanarata

et al. 2015

IJN

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The effect of low frequency sonophoresis (SN, 20 kHz) on the skin transport of sodium fluorescein (NaFI)-loaded liposomes was investigated. An in vitro skin penetration study in open and blocked hair follicles was performed, and confocal laser scanning microscopy and scanning electron microscopy were used to visualize the penetration pathways. The results showed that SN significantly increased the flux of NaFI solution, whereas it significantly decreased the flux of NaFI-loaded polyethylene glycol-coated (PEGylated) liposomes with D-limonene (PL-LI). SN did not significantly affect the flux of NaFI-loaded conventional liposomes and PEGylated liposomes. In the blocked follicles, the flux of NaFI-loaded PL-LI both with and without SN decreased, indicating that NaFI-loaded PL-LI penetrated the skin via the transfollicular pathway. A confocal laser scanning microscopy image showed that in the skin without SN, the fluorescence intensity of NaFI-loaded PL-LI was observed in the skin and along the length of hair inside the skin, whereas in the skin with applied SN, the fluorescence intensity was detected only on the top of hair outside the skin. From scanning electron microscopy images, SN dislocated the corneocytes and reduced the deposition of PL-LI around hair follicles. These results revealed that SN may partially plug hair follicle orifices and reduce percutaneous absorption through the follicular pathway.

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“…Evidence suggests that topically applied compounds entrapped in liposomes accumulated not only in the HF, but also in the sebaceous glands [159]. While the presence of lipophilic sebum may favor follicular uptake of lipophilic molecules, sebum production may, however, moderate drug transport, especially for hydrophilic drugs, functioning as a physical and a chemical barrier for drug penetration [160].…”

Section: Treatments Of Hair Growth Disorders: Room For Improvementmentioning

confidence: 99%

Biology of Human Hair: Know Your Hair to Control It

Araújo

Fernandes

Cavaco‐Paulo

et al. 2010

Advances in Biochemical Engineering/Biotechnology

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Hair can be engineered at different levels-its structure and surfacethrough modification of its constituent molecules, in particular proteins, but also the hair follicle (HF) can be genetically altered, in particular with the advent of siRNA-based applications. General aspects of hair biology are reviewed, as well as the most recent contributions to understanding hair pigmentation and the regulation of hair development. Focus will also be placed on the techniques developed specifically for delivering compounds of varying chemical nature to the HF, indicating methods for genetic/biochemical modulation of HF components for the treatment of hair diseases. Finally, hair fiber structure and chemical characteristics will be discussed as targets for keratin surface functionalization.

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Transfollicular drug delivery—Is it a reality?

Cited by 139 publications

References 66 publications

Noninvasive and persistent transfollicular drug delivery system using a combination of liposomes and iontophoresis

Noninvasive and persistent transfollicular drug delivery system using a combination of liposomes and iontophoresis

Mechanistic study of decreased skin penetration using a combination of sonophoresis with sodium fluorescein-loaded PEGylated liposomes with D-limonene

Biology of Human Hair: Know Your Hair to Control It

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