Improvement of the skin penetration of hydrophobic drugs by polymeric micelles

Yotsumoto, Kensuke; Ishii, Kenta; Kokubo, Miho; Yasuoka, Sakiko

doi:10.1016/j.ijpharm.2018.10.039

Cited by 39 publications

(29 citation statements)

References 31 publications

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“…DSPE-PEG micelles have shown to be a potential drug carrier, 27 increasing apparent aqueous solubility and enhancing cutaneous penetration of hydrophobic drugs. [28][29][30] We have hypothesized that associated with LFU, this micellar system can yet facilitate the cavitation process because of the co-polymer surface properties, 31 improving the creation of transient pathways in the skin and facilitating the penetration of the sensitizing agent. Moreover, we investigate for the first time, the potential of the LFU irradiation of ZnPc-loaded micelles in submit your manuscript | www.dovepress.com…”

Section: Introductionmentioning

confidence: 99%

<p>Bifunctional Therapeutic Application of Low-Frequency Ultrasound Associated with Zinc Phthalocyanine-Loaded Micelles</p>

Martins¹,

Fonseca²,

Pavan³

et al. 2020

IJN

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Purpose: Sonodynamic therapy (SDT) is a new therapeutic modality for the noninvasive cancer treatment based on the association of ultrasound and sonosensitizer drugs. Topical SDT requires the development of delivery systems to properly transport the sonosensitizer, such as zinc phthalocyanine (ZnPc), to the skin. In addition, the delivery system itself can participate in sonodynamic events and influence the therapeutic response. This study aimed to develop ZnPc-loaded micelle to evaluate its potential as a topical delivery system and as a cavitational agent for low-frequency ultrasound (LFU) application with the dual purpose of promoting ZnPc skin penetration and generating reactive oxygen species (ROS) for SDT. Methods: ZnPc-loaded micelles were developed by the thin-film hydration method and optimized using the Quality by Design approach. Micelles' influence on LFU-induced cavitation activity was measured by potassium iodide dosimeter and aluminum foil pits experiments. In vitro skin penetration of ZnPc was assessed after pretreatment of the skin with LFU and simultaneous LFU treatment using ZnPc-loaded micelles as coupling media followed by 6 h of passive permeation of ZnPc-loaded micelles. The singlet oxygen generation by LFU irradiation of the micelles was evaluated using two different hydrophilic probes. The lipid peroxidation of the skin was estimated using the malondialdehyde assay after skin treatment with simultaneous LFU using ZnPc-loaded micelles. The viability of the B16F10 melanoma cell line was evaluated using resazurin after treatment with different concentrations of ZnPc-loaded micelles irradiated or not with LFU. Results: The micelles increased the solubility of ZnPc and augmented the LFU-induced cavitation activity in two times compared to water. After 6 h ZnPc-loaded micelles skin permeation, simultaneous LFU treatment increased the amount of ZnPc in the dermis by more than 40 times, when compared to non-LFU-mediated treatment, and by almost 5 times, when compared to LFU pretreatment protocol. The LFU irradiation of micelles induced the generation of singlet oxygen, and the lipoperoxidation of the skin treated with the simultaneous LFU was enhanced in three times in comparison to the non-LFU-treated skin. A significant reduction in cell viability following treatment with ZnPc-loaded micelles and LFU was observed compared to blank micelles and non-LFU-treated control groups. Conclusion: LFU-irradiated mice can be a potential approach to skin cancer treatment by combining the functions of increasing drug penetration and ROS generation required for SDT.

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Section: Introductionmentioning

confidence: 99%

<p>Bifunctional Therapeutic Application of Low-Frequency Ultrasound Associated with Zinc Phthalocyanine-Loaded Micelles</p>

Martins¹,

Fonseca²,

Pavan³

et al. 2020

IJN

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“…Bioactive agents which are incorporated into the core of the polymeric micelles include charged compounds, lipophilic substances and metal complexes. Micelles are structurally stable even at low concentrations [ 32 ].…”

Section: Application Of Cholesterol-based Carriers In Anticancer Dmentioning

confidence: 99%

The Efficacy of Cholesterol-Based Carriers in Drug Delivery

Ruwizhi

Aderibigbe

2020

Molecules

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Several researchers have reported the use of cholesterol-based carriers in drug delivery. The presence of cholesterol in cell membranes and its wide distribution in the body has led to it being used in preparing carriers for the delivery of a variety of therapeutic agents such as anticancer, antimalarials and antivirals. These cholesterol-based carriers were designed as micelles, nanoparticles, copolymers, liposomes, etc. and their routes of administration include oral, intravenous and transdermal. The biocompatibility, good bioavailability and biological activity of cholesterol-based carriers make them potent prodrugs. Several in vitro and in vivo studies revealed cholesterol-based carriers potentials in delivering bioactive agents. In this manuscript, a critical review of the efficacy of cholesterol-based carriers is reported.

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“…[4,8,31,78]. In the absence of any activation mechanism, penetration of the skin by the therapeutic agent released from the dermal delivery system is determined by its solubility and diffusivity through the stratum corneum [91], it depends on certain intrinsic properties of the molecule. For example, the aqueous solubility of a non-ionized organic compound is related to its octanol-water partition coefficient (P) [43], and is correlated with its melting point (MP) [62].…”

Section: Introductionmentioning

confidence: 99%

Compatibility Study of Four Binary Combinations of Active Ingredients for Dermal Film Forming Systems

Rusu¹

2020

FARMACIA

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Adapalene (ADA), levofloxacin (LEV), meloxicam (MEL) and miconazole nitrate (MIC) were selected as potential active ingredients for film systems with dermal or transdermal delivery. This study aimed to evaluate the compatibility of four binary mixtures-ADA and LEV (M1), ADA and MIC (M2), LEV and MEL (M3), and LEV and MIC (M4)combinations for new bioadhesive polymeric matrix dermal systems produced by the casting solvent evaporation technique. The Fouriertransform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and molecular modelling (MM) were used to characterise and evaluate the compatibility between the selected active substances. In the FTIR data, M1, M2, and M4 mixtures presented a good compatibility. DSC revealed different chemical interactions as the temperature rose above 160°C, especially for M3 and M4. Through MM technique, interactions were found on the M2 and M3 mixtures. Following the correlation of all obtained results, the best compatibility was found to be on M1 and M4 combinations. Rezumat Adapalenul (ADA), levofloxacina (LEV), meloxicamul (MEL) şi nitratul de miconazol (MIC) au fost selectate ca potenţiale ingrediente active în sistemele de tip film cu eliberare dermică sau transdermică. Scopul acestui studiu este de a evalua compatibilitatea a patru amestecuri binare-ADA şi LEV (M1), ADA şi MIC (M2), LEV şi MEL (M3), şi LEV şi MIC (M4)-combinaţii pentru noi sisteme dermice de tip matriţă polimerică bioadezivă produse prin tehnica de turnare şi evaporare a solventului. Pentru a caracteriza şi evalua compatibilitatea dintre substanţele active selectate au fost utilizate spectroscopia cu transformată Fourier (FTIR), calorimetria cu scanare diferenţială (DSC) şi modelarea moleculară (MM). Din datele FTIR, amestecurile M1, M2 şi M4 au fost compatibilite. DSC a arătat diferite interacţiuni chimice, în special pentru M3 şi M4, la temperaturi mai mari de 160°C. Prin metoda MM au fost semnalate interacţiuni în combinaţiile M2 şi M3. Ca urmare a corelării tuturor rezultatelor obţinute, cea mai bună compatibilitate a fost găsită în combinaţiile M1 şi M4.

show abstract

Improvement of the skin penetration of hydrophobic drugs by polymeric micelles

Cited by 39 publications

References 31 publications

<p>Bifunctional Therapeutic Application of Low-Frequency Ultrasound Associated with Zinc Phthalocyanine-Loaded Micelles</p>

<p>Bifunctional Therapeutic Application of Low-Frequency Ultrasound Associated with Zinc Phthalocyanine-Loaded Micelles</p>

The Efficacy of Cholesterol-Based Carriers in Drug Delivery

Compatibility Study of Four Binary Combinations of Active Ingredients for Dermal Film Forming Systems

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