Physical Enhancement? Nanocarrier? Current Progress in Transdermal Drug Delivery

Uchida, Noriyuki; Yanagi, Masayoshi; Hamada, Hiroki

doi:10.3390/nano11020335

Cited by 23 publications

(19 citation statements)

References 108 publications

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“…Though the ZP value of F2 was higher than F4, the cumulative amount of drug absorbed from F4 was higher than that of F2, this can be attributed to the higher HLB value of PF127 than that of T80 (22, 15; respectively). In case of F1, the enhancement of drug permeation was compromised between two antagonizing factors including the thin shape of the formed discs along with their smaller size which enhance their ability to penetrate and pass the narrow gaps ( 57 ), at the same time the incomplete drug absorption can be attributed to the lower negative ZP value of the formula (-6.8±0.5). It is noteworthy to point to the role of the 20 % free PEG content of labrasol in interacting with and shielding of the phosphate group of the bicelles hydrophilic heads and hence decreasing the ZP value of F1.…”

Section: Resultsmentioning

confidence: 99%

Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19

et al. 2021

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Investigating bicelles as an oral drug delivery system and exploiting their structural benefits can pave the way to formulate hydrophobic drugs and potentiate their activity. Herein, the ability of non-ionic surfactants (labrasol®, tween 80, cremophore EL and pluronic F127) to form curcumin loaded bicelles with phosphatidylcholine, utilizing a simple method, was investigated. Molecular docking was used to understand the mechanism of bicelles formation. The % transmittance and TEM exhibited bicelles formation with labrasol® and tween 80, while cremophor EL and pluronic F127 tended to form mixed micelles. The surfactant-based nanostructures significantly improved curcumin dissolution (99.2 ± 2.6% within 10 min in case of tween 80-based bicelles) compared to liposomes and curcumin suspension in non-sink conditions. The prepared formulations improved curcumin ex vivo permeation over liposomes and drug suspension. Further, the therapeutic antiviral activity of the formulated curcumin against SARS-CoV-2 was potentiated over drug suspension. Although both Labrasol® and tween 80 bicelles could form bicelles and enhance the oral delivery of curcumin when compared to liposomes and drug suspension, the mixed micelles formulations depicted superiority than bicelles formulations. Our findings provide promising formulations that can be utilized for further preclinical and clinical studies of curcumin as an antiviral therapy for COVID-19 patients.

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Section: Resultsmentioning

confidence: 99%

Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19

et al. 2021

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“…Transdermal delivery as a non-invasive route of drug administration has been widely used for the treatment of skin disorders, allowing for rapid, pain-free administration either by minimally trained healthcare providers or through self-administration 247 . Moreover, drug delivery via the transdermal route can avoid first-pass elimination and digestive enzyme metabolism.…”

Section: Mdps-based Formulations and Their Applicationsmentioning

confidence: 99%

Membrane-disruptive peptides/peptidomimetics-based therapeutics: Promising systems to combat bacteria and cancer in the drug-resistant era

Lin

Chi

Yan

et al. 2021

Acta Pharmaceutica Sinica B

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Membrane-disruptive peptides/peptidomimetics (MDPs) are antimicrobials or anticarcinogens that present a general killing mechanism through the physical disruption of cell membranes, in contrast to conventional chemotherapeutic drugs, which act on precise targets such as DNA or specific enzymes. Owing to their rapid action, broad-spectrum activity, and mechanisms of action that potentially hinder the development of resistance, MDPs have been increasingly considered as future therapeutics in the drug-resistant era. Recently, growing experimental evidence has demonstrated that MDPs can also be utilized as adjuvants to enhance the therapeutic effects of other agents. In this review, we evaluate the literature around the broad-spectrum antimicrobial properties and anticancer activity of MDPs, and summarize the current development and mechanisms of MDPs alone or in combination with other agents. Notably, this review highlights recent advances in the design of various MDP-based drug delivery systems that can improve the therapeutic effect of MDPs, minimize side effects, and promote the co-delivery of multiple chemotherapeutics, for more efficient antimicrobial and anticancer therapy.

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“…Among the most widely used chemical permeability enhancers are ethanol, unsaturated fatty acids, surfactants, and terpenoids. Flexible liposomes prepared with phospholipids and surfactant were once thought to transport encapsulated drugs across the stratum corneum by squeezing through the intercellular spaces; however, it is now thought that the surfactant permeabilizes the intercellular lamellae to enhance drug flux [ 66 ]. There may also be increased hydration of the stratum corneum, which would increase permeability.…”

Section: Transdermal Drug Deliverymentioning

confidence: 99%

Roles of Lipids in the Permeability Barriers of Skin and Oral Mucosa

Wertz

2021

IJMS

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PubMed searches reveal much literature regarding lipids in barrier function of skin and less literature on lipids in barrier function of the oral mucosa. In terrestrial mammals, birds, and reptiles, the skin’s permeability barrier is provided by ceramides, fatty acids, and cholesterol in the outermost layers of the epidermis, the stratum corneum. This layer consists of about 10–20 layers of cornified cells embedded in a lipid matrix. It effectively prevents loss of water and electrolytes from the underlying tissue, and it limits the penetration of potentially harmful substances from the environment. In the oral cavity, the regions of the gingiva and hard palate are covered by keratinized epithelia that much resemble the epidermis. The oral stratum corneum contains a lipid mixture similar to that in the epidermal stratum corneum but in lower amounts and is accordingly more permeable. The superficial regions of the nonkeratinized oral epithelia also provide a permeability barrier. These epithelial regions do contain ceramides, cholesterol, and free fatty acids, which may underlie barrier function. The oral epithelial permeability barriers primarily protect the underlying tissue by preventing the penetration of potentially toxic substances, including microbial products. Transdermal drug delivery, buccal absorption, and lipid-related disease are discussed.

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Physical Enhancement? Nanocarrier? Current Progress in Transdermal Drug Delivery

Cited by 23 publications

References 108 publications

Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19

Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19

Membrane-disruptive peptides/peptidomimetics-based therapeutics: Promising systems to combat bacteria and cancer in the drug-resistant era

Roles of Lipids in the Permeability Barriers of Skin and Oral Mucosa

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