I have been studying the improvement of drug solubility using solid dispersion and skin-applied formulations. When preparing solid dispersions using phosphatidylcoline (PC) as a carrier, drug with hydrogen-donating groups interacts with PC to produce amorphous solid dispersions with high drug content; this overcomes improves drug absorption. The drug was solubilized and supersaturated in the oil-based gel formed with hyadrogenated lecithin; this facilitates drug permeation through the skin. The promoting effect differs with the nature of the oil used because of the skin penetration of the oil itself and the accompanying increase in drug solubility and diffusion coefficient in the skin. At actual application volumes of 10 µL/cm or less, the skin penetration of poorly-absorbable drugs depends on the molecular weight and surface tension of the oil. The penetration of the oil vehicle into the upper stratum corneum influences the reach of the drug into the stratum corneum; a high drug concentration near the 7th layer of the stratum corneum promotes migration through the skin by increasing the linear concentration gradient in deeper layers. In addition, we performed a risk assessment, in collaboration with toxicologists, for dermal safety that included the toxicity potential of substances and the parts related to skin transfer.
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http://dx.doi.org/10.1248/yakushi.23-00155 | DOI Listing |
Small
January 2025
Department of Clinical Pharmacology, The Second Hospital of Anhui Medical University, Anhui Medical University, Hefei, 230601, P. R. China.
Topical transdermal drug delivery for psoriasis remains a challenge because of the poor solubility of hydrophobic drugs and the limited penetration of the stratum corneum. In this study, a near-infrared (NIR) light-responsive thermosensitive hydrogel (PDLLA-PEG-PDLLA, PLEL)-based drug reservoir is developed that directly incorporated gold nanorods (GNRs) and methotrexate (MTX) in the sol state at low temperature, which is referred to as PLEL@GNR+MTX. The in vitro anti-psoriasis experiment indicated that, GNRs, as photothermal cores of composite hydrogel, not only triggered keratinocyte apoptosis but also promoted MTX release in a synergistic manner.
View Article and Find Full Text PDFAAPS PharmSciTech
January 2025
Department of Pharmaceutics, School of Pharmaceutical Science, Siksha 'O' Anusandhan University, Bhubaneswar, 751003, Odisha, India.
Transdermal drug delivery (TDD) represents a transformative paradigm in drug administration, offering advantages such as controlled drug release, enhanced patient adherence, and circumvention of hepatic first-pass metabolism. Despite these benefits, the inherent barrier function of the skin, primarily attributed to the stratum corneum, remains a significant impediment to the efficient permeation of therapeutic agents. Recent advancements have focused on macromolecular-assisted permeation enhancers, including carbohydrates, lipids, amino acids, nucleic acids, and cell-penetrating peptides, which modulate skin permeability by transiently altering its structural integrity.
View Article and Find Full Text PDFAdv Sci (Weinh)
January 2025
Dermatology Hospital, Southern Medical University, Guangzhou, 510091, China.
Sigal peptides have garnered remarkable efficacy in rejuvenating photoaged skin and delaying senescence. Nevertheless, their low solubility and poor permeability bring about a formidable challenge in their transdermal delivery. To address this challenge, bioactive ionic liquids (ILs) synthesized from natural glycyrrhizic acid (GA) and oxymatrine (OMT) with eminent biocompatibility is first prepared.
View Article and Find Full Text PDFJ Cosmet Dermatol
January 2025
Cosmetic Science, Institute of Biochemistry and Molecular Biology, University of Hamburg, Hamburg, Germany.
Background: The concept of "skin quality" (SQ) has gained widespread attention, with a recent international consensus defining it and outlining four "emergent perceptual categories" (EPCs), each accompanied by specific parameters and associated measurement methods. No research has confirmed whether the parameters linked to these EPCs vary objectively with age. This gap in data is significant, as understanding how these parameters correlate with age could be essential for creating an objective, age-adjusted classification of SQ.
View Article and Find Full Text PDFAssay Drug Dev Technol
January 2025
University Institute of Pharmacy, Pandit Ravishankar Shukla University, Raipur, India.
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