Percutaneous Absorption and Antibacterial Activities of Lipid Nanocarriers Loaded with Dual Drugs for Acne Treatment

Lin, Cheng-Kuo; Fang, Yi‐Ping; Al‐Suwayeh, Saleh A.; Yang, Shih-Yung; Fang, Jia‐You

doi:10.1248/bpb.b12-00793

Cited by 33 publications

(15 citation statements)

References 47 publications

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“…The permeant amount within skin reservoir was extracted by methanol for tretinoin and estradiol or 0.1 N HCl for dextran as described previously (Hsieh et al 2013). The samples of tretinoin and estradiol were analyzed by high performance liquid chromatography (HPLC) (Fang et al 2001;Lin et al 2013). The samples taken from dextran application were quantified by a fluorescence spectrophotometer (F2500, Hitachi, Tokyo, Japan).…”

Section: In Vitro Percutaneous Absorptionmentioning

confidence: 99%

Skin aging modulates percutaneous drug absorption: the impact of ultraviolet irradiation and ovariectomy

Hung

Chen

Aljuffali

et al. 2015

AGE

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Ultraviolet (UV) exposure and menopause are known as the inducers of damage to the skin structure. The combination of these two factors accelerates the skin aging process. In this study, we aimed to evaluate the influence of UVand ovariectomy (OVX) on the permeation of drugs through the skin. The role of tight junctions (TJs) and adherens junctions (AJs) in the cutaneous absorption of extremely lipophilic permeants and macromolecules was explored. The OVX nude mouse underwent bilateral ovary removal. Both UVA and UVB were employed to irradiate the skin. The physiological and biochemical changes of the skin structure were examined with focus on transepidermal water loss (TEWL), skin color, immunohistochemistry, and mRNA levels of proteins. UVB and OVX increased TEWL, resulting in stratum corneum (SC) integrity disruption and dehydration. A hyperproliferative epidermis was produced by UVB. UVA caused a pale skin color tone due to keratinocyte apoptosis in the epidermis. E-cadherin and β-catenin showed a significant loss by both UVA and UVB. OVX downregulated the expression of filaggrin and involucrin. A further reduction was observed when UV and OVX were combined. The in vitro cutaneous absorption demonstrated that UV AGE (2015) increased the skin permeation of tretinoin by about twofold. However, skin accumulation and flux of estradiol were not modified by photoaging. OVX basically revealed a negligible effect on altering the permeation of small permeants. OVX increased tretinoin uptake by the appendages from 1.36 to 3.52 μg/cm 2 . A synergistic effect on tretinoin follicular uptake enhancement was observed for combined UV and OVX. However, the intervention of OVX to photoaged skin resulted in less macromolecule (dextran, molecular weight=4 kDa) accumulation in the skin reservoir because of retarded partitioning into dry skin. The in vivo percutaneous absorption of lipophilic dye examined by confocal microscopy had indicated that the SC was still important to controlling topical delivery, although the role of epidermal junctions could not be simply ignored.

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Section: In Vitro Percutaneous Absorptionmentioning

confidence: 99%

Skin aging modulates percutaneous drug absorption: the impact of ultraviolet irradiation and ovariectomy

Hung

Chen

Aljuffali

et al. 2015

AGE

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“…Since drug molecule basically did not influence the zeta potential (data not shown) and Polysorbate 80 is a non-ionic surfactant, the some ionization and/or hydrolysis of fatty ester groups in Labrafil M1944CS and/or Precirol ATO 5 was possibly responsible for the negative surface charge. 21) According to the literature, when the absolute value of zeta potential for colloidal system is higher than 30 mV, the particles are electrochemically stable under the storage condition because the surface charge prevents aggregation of the particles. 22,23) The NLC aqueous dispersion system showed a high loading efficiency greater than 86%, which indicated that VRC was efficiently incorporated into the lipid particles with their lipophilicity (Log P value of 1.8).…”

Section: Vrc Assay Validationmentioning

confidence: 99%

Improved Skin Delivery of Voriconazole with a Nanostructured Lipid Carrier-Based Hydrogel Formulation

et al. 2014

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In order to develop topical preparations of voriconazole (VRC) for the treatment of mycotic infections of the skin, a nanostructured lipid carrier-based hydrogel (NLC-gel) formulation was developed and its physical characteristics, in vitro skin permeation, and retention profiles were examined. A VRC-loaded NLC dispersion, consisting of Precirol ATO 5, Labrafil 1944 CS, and Tween 80, was prepared by high-pressure homogenization and embedded into Carbopol 940 hydrogel. The lipid nanoparticles in the hydrogel were approximately 210 nm in size, with a spherical shape and zeta potential of 30 mV. In a skin permeation study using a Franz diffusion cell mounted with depilated mouse skin, the NLC-gel was superior to conventional cream and microemulsion-based gel formulations, showing 2.8-and 1.7-fold greater flux values, respectively. In addition, the NLC-gel led to markedly greater accumulation of VRC in deeper skin layers as compared with the reference formulations. In conclusion, the novel topical formulation reported here represents an alternative treatment for skin infections such as candidiasis, with less potential for systemic adverse effects than oral therapy.Key words voriconazole; nanostructured lipid carrier; hydrogel; topical delivery Voriconazole (VRC), a second-generation triazole derived from fluconazole, is a broad-spectrum anti-fungal agent that inhibits cytochrome P450-dependent 14α-lanosterol demethylation, which is a vital step in cell membrane ergosterol synthesis.1) VRC is active against all Candida species that have acquired resistance to fluconazole and is currently used for the treatment of aspergillosis and candidiasis infections in the abdomen, kidney, bladder wall, wounds, and skin.1,2) Despite its advantageous pharmacological activity, systemic exposure to VRC as a result of oral and/or intravenous administration can cause several side effects, not fatal but considerable, including photopsia, abdominal pain, and visual hallucinations.3,4) In addition, VRC triggers elevations in hepatic enzyme levels in patients at a high risk of pharmacokinetic drug-drug interactions. 4)A need exists for a topical delivery system for VRC to overcome limitations in oral and intravenous treatment, and which will be particularly useful against candidiasis in wounds and skin tissue. Topical drug application provides higher local tissue levels, more rapid drug delivery, and lower systemic exposure than oral administration. 5) However, because of the poor aqueous solubility of VRC, 6) solubilization of the drug is necessary for delivery in a topical formulation. Furthermore, a penetration-enhancing system is required to achieve therapeutic concentrations in stratum corneum and deeper skin layers, including epidermis and/or dermis.In recent years, nanostructured lipid carriers (NLC) have emerged as a promising topical delivery system for pharmaceutical and cosmetic molecules, especially for the delivery of lipophilic compounds. 7-9) NLC dispersions composed of a solid lipid matrix with a liquid-lipid are colloidal...

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“…Precirol, composed of fatty esters, possessed amphiphilic properties (20). The surface-active esters could assist in the emulsification process for reducing particle size and creating a rigid interface.…”

Section: Discussionmentioning

confidence: 99%

Squarticles as a Lipid Nanocarrier for Delivering Diphencyprone and Minoxidil to Hair Follicles and Human Dermal Papilla Cells

Aljuffali

Sung

Shen

et al. 2013

AAPS J

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Abstract. Delivery of diphencyprone (DPCP) and minoxidil to hair follicles and related cells is important in the treatment of alopecia. Here we report the development of "squarticles," nanoparticles formed from sebum-derived lipids such as squalene and fatty esters, for use in achieving targeted drug delivery to the follicles. Two different nanosystems, nanostructured lipid carriers (NLC) and nanoemulsions (NE), were prepared. The physicochemical properties of squarticles, including size, zeta potential, drug encapsulation efficiency, and drug release, were examined. Squarticles were compared to a free control solution with respect to skin absorption, follicular accumulation, and dermal papilla cell targeting. The particle size of the NLC type was 177 nm; that of the NE type was 194 nm. Approximately 80% of DPCP and 60% of minoxidil were entrapped into squarticles. An improved drug deposition in the skin was observed in the in vitro absorption test. Compared to the free control, the squarticles reduced minoxidil penetration through the skin. This may indicate a minimized absorption into systemic circulation. Follicular uptake by squarticles was 2-and 7-fold higher for DPCP and minoxidil respectively compared to the free control. Fluorescence and confocal images of the skin confirmed a great accumulation of squarticles in the follicles and the deeper skin strata. Vascular endothelial growth factor expression in dermal papilla cells was significantly upregulated after the loading of minoxidil into the squarticles. In vitro papilla cell viability and in vivo skin irritancy tests in nude mice suggested a good tolerability of squarticles to skin. Squarticles provide a promising nanocarrier for topical delivery of DPCP and minoxidil.

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Percutaneous Absorption and Antibacterial Activities of Lipid Nanocarriers Loaded with Dual Drugs for Acne Treatment

Cited by 33 publications

References 47 publications

Skin aging modulates percutaneous drug absorption: the impact of ultraviolet irradiation and ovariectomy

Skin aging modulates percutaneous drug absorption: the impact of ultraviolet irradiation and ovariectomy

Improved Skin Delivery of Voriconazole with a Nanostructured Lipid Carrier-Based Hydrogel Formulation

Squarticles as a Lipid Nanocarrier for Delivering Diphencyprone and Minoxidil to Hair Follicles and Human Dermal Papilla Cells

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