Article
Pharmacology & Pharmacy
Ekaterina P. Vasyuchenko, Philipp S. Orekhov, Grigoriy A. Armeev, Marine E. Bozdaganyan
Summary: The cutaneous delivery route is increasingly common for drug administration, with the use of chemical penetration enhancers (CPEs) to facilitate drug transport through skin layers. The creation of a CPE-DB database allows for the classification and identification of new enhancers, as well as the prediction of biological activity using machine-learning applications.
Review
Pharmacology & Pharmacy
Victor Hmingthansanga, Nidhi Singh, Superna Banerjee, Sivakumar Manickam, Ravichandiran Velayutham, Subramanian Natesan
Summary: Delivery of drugs via transdermal routes offers advantages, but overcoming the skin's barrier properties remains challenging. Chemical permeation enhancers (CPEs) can improve transdermal drug delivery, but may have side effects. With advancements in analytical techniques, synthetic chemistry, and combinatorial studies, CPEs-aided transdermal drug delivery is expected to reach its full potential.
Article
Pharmacology & Pharmacy
Lijuan Zeng, Guangqiang Yang, Jianping Liu, Danyi Quan, Wenting Song
Summary: This study investigated the dynamic behavior of chemical enhancers (CEs) in enhancing drug permeation by studying the processes of passing in, acting on, and passing out of the stratum corneum. The rate of CEs passing in and out of the SC was found to be dependent on their affinity with the SC and their interaction with it. The study confirmed the relevance between CEs' dynamic behavior and the extent of decreasing the SC barrier, leading to a potential for more effectively enhancing drug permeation.
Article
Chemistry, Multidisciplinary
Nikolett Kis, Maria Gunnarsson, Szilvia Berko, Emma Sparr
Summary: The skin provides an attractive alternative to conventional drug administration routes, but the stratum corneum (SC) presents challenges as an efficient barrier to most compounds. This study investigates the molecular effects of three types of glycols in the SC, aiming to understand their influence on molecular mobility and structure, as well as their efficiency as permeation enhancers. The results show that all three glycols increase lipid mobility in the SC and have permeation enhancing effects. There is also a non-monotonic response in permeation enhancement with respect to glycol concentration.
JOURNAL OF CONTROLLED RELEASE
(2022)
Article
Biochemistry & Molecular Biology
Sofia A. Costa Lima, Ana Isabel Barbosa, Claudia Nunes, Ibraheem Yousef, Salette Reis
Summary: The application of nanoparticles as permeation enhancers in skin drug delivery is a growing research field. This study used synchrotron-based Fourier Transform Infrared Microspectroscopy (SR-FTIRM) combined with multivariate analysis and in vitro skin permeation assay to elucidate the mechanisms of nanoparticles' interaction with the skin structure. The findings reveal molecular changes in the skin structure induced by fucoidan/chitosan nanoparticles, which enhance skin permeation. These findings are important for designing nanoparticles to determine their fate within the skin structure.
CHEMISTRY AND PHYSICS OF LIPIDS
(2022)
Article
Biochemistry & Molecular Biology
Charlotte M. Beddoes, Denise E. Rensen, Gert S. Gooris, Marc Malfois, Joke A. Bouwstra
Summary: The study found that the effects of FFA chain lengths on lamellar phases and lateral packing vary, with a threshold for water permeability at FFA C16.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Marine E. Bozdaganyan, Philipp S. Orekhov
Summary: The study used molecular dynamics simulations to investigate the effects of two chemical penetration enhancers (CPEs) on lidocaine delivery through the stratum corneum (SC) model membrane. It was found that the combination of linoleic acid (LA) and ethanol decreased membrane thickness, altered hydrocarbon chain order parameters, and enhanced diffusion. The simulations also showed that ethanol reduced the free energy barrier, while LA decreased the depth of the free energy minima for lidocaine translocation across SC, resulting in a synergistic penetration enhancement effect.
Article
Chemistry, Medicinal
Shweta Ramkar, Monika Kaurav, M. S. Sudheesh, Ravi Shankar Pandey
Summary: DMSO-modified liposomes were prepared to enhance the topical delivery of finasteride (FIN) for the treatment of androgenic alopecia. The permeation-enhancing property of DMSO was utilized to promote drug delivery to deeper skin layers where hair follicles are present. The optimized DMSO-liposomes showed promising biological effects in a rat model of testosterone-induced alopecia.
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
(2023)
Article
Biochemistry & Molecular Biology
Nozomi Honma, Ichiro Hatta, Toshiro Okazaki, Yoshihiro Tokudome
Summary: The study reveals that deficiency of sphingomyelin synthase (SMS) leads to a decrease in the barrier function and changes in the lamellar structure of the stratum corneum (SC). The permeability of hydrophilic compounds is significantly increased in the skin of SMS2-knockout (KO) mice, while there is no difference in the penetration of lipophilic compounds. X-ray diffraction analysis shows the presence of highly ordered structures in the SC of SMS2-KO mice, suggesting a potential cause for the reduced barrier function of the skin.
CHEMISTRY AND PHYSICS OF LIPIDS
(2022)
Article
Toxicology
Benjamin N. Deacon, Nicola Piasentin, Qiong Cai, Tao Chen, Guoping Lian
Summary: Permeability and partition coefficients of the skin barrier are important for evaluating the absorption and safety of cosmetics and medicine. This study analyzes the relationship between skin permeability and hydrophobicity using the Potts and Guy equation and identifies significant differences in published datasets. The weak correlation and dependence of the late permeability datasets with skin lipid/water partition suggest the presence of additional non-lipid pathways or a weaker skin barrier property.
TOXICOLOGY IN VITRO
(2023)
Article
Chemistry, Multidisciplinary
Yogesh Badhe, Pradyumn Sharma, Rakesh Gupta, Beena Rai
Summary: The interactions between two types of nanoparticles (bare and dodecane-thiol coated) and skin lipid membranes were studied using coarse-grained MARTINI molecular dynamics simulations. The nanoparticles were found to exist in the lipid membrane as individual entities or clusters, regardless of their type and concentration. Coated nanoparticles exhibited higher penetration across the double bilayer membrane and formed a single large cluster inside the membrane, while bare nanoparticles formed smaller clusters. Both types of nanoparticles showed preferential interactions with cholesterol molecules in the lipid membrane. A minimum double bilayer model should be used for translocation studies due to the unrealistic instability of the single membrane model at moderate to higher nanoparticle concentrations.
NANOSCALE ADVANCES
(2023)
Article
Polymer Science
Asif Nawaz, Arshad Farid, Muhammad Safdar, Muhammad Shahid Latif, Shakira Ghazanfar, Nosheen Akhtar, Soad K. Al Jaouni, Samy Selim, Muhammad Waseem Khan
Summary: This research developed a curcumin hydrogel containing natural essential oils as permeation enhancers and demonstrated that suitable natural permeation enhancers can improve the in vitro release and ex vivo permeation and retention of curcumin. Among various natural essential oils, 3% aloe vera oil had the greatest effect on the permeability rate and skin retention of curcumin.
Article
Pharmacology & Pharmacy
Akeemat O. O. Tijani, Dorcas Frempong, Jagroop Kaur, Sophia Sergent, Kara Shaw, Rebecca Lessaint, Maryam Al Shawi, Gabrielle Verana, Ashana Puri
Summary: In this study, the effect of dermaplaning, a popular skin rejuvenation technique, on drug permeation was investigated. The removal of stratum corneum and viable epidermis was observed after dermaplaning. Significant drug flux and permeation were observed for the model drugs across dermaplaned skin. However, the absorption profile varied for both drugs, with dermaplaning displaying better suitability for enhancing the permeation of the hydrophilic drug.
Article
Biochemistry & Molecular Biology
Akihiro Watari, Kana Fujiwara, Kiyohito Yagi, Keisuke Tachibana, Takeshi Katsurada, Akira Myoui, Masuo Kondoh
Summary: The study shows that HHT may serve as a granular permeation enhancer by altering the TJ molecules in epidermal cells to enhance transdermal absorption of dextran.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2022)
Article
Multidisciplinary Sciences
Chao-Chun Yang, Yun-Yo Yen, Chao-Kai Hsu, Nan-Yu Cheng, Shih-Yu Tzeng, Shih-Jay Chou, Jun-Ming Chang, Sheng-Hao Tseng
Summary: This study investigated near infrared spectroscopic features of psoriatic and normal skin, revealing significant differences that could be linked to the epidermal barrier function. It was found that using diffuse reflectance spectroscopy could achieve objective evaluation of the epidermal barrier function of psoriasis.
SCIENTIFIC REPORTS
(2021)
Review
Biotechnology & Applied Microbiology
Taksim Ahmed, Amany O. Kamel, Shawn D. Wettig
Article
Chemistry, Physical
Tahereh Fereidooni Moghadam, Saeid Azizian, Shawn Wettig
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2017)
Article
Chemistry, Physical
Samantha M. Shortall, Shawn D. Wettig
JOURNAL OF PHYSICAL CHEMISTRY B
(2018)
Article
Chemistry, Physical
Aula Al Muslim, Dana Ayyash, Sarbjeet Singh Gujral, George M. Mekhail, Praveen P. N. Rao, Shawn D. Wettig
PHYSICAL CHEMISTRY CHEMICAL PHYSICS
(2017)
Article
Chemistry, Physical
M. S. Islam, S. M. Shortall, G. M. Mekhail, S. P. Callender, O. Madkhali, Z. Bharwani, D. Ayyash, K. Kobernyk, S. D. Wettig
PHYSICAL CHEMISTRY CHEMICAL PHYSICS
(2017)
Article
Nanoscience & Nanotechnology
Shruti Nambiar, Ernest Osei, Andre Fleck, Johnson Darko, Anthony J. Mutsaers, Shawn Wettig
APPLIED NANOSCIENCE
(2018)
Review
Pharmacology & Pharmacy
Osama Madkhali, George Mekhail, Shawn D. Wettig
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2019)
Article
Chemistry, Multidisciplinary
Luzhu Xu, Adam R. Tetreault, Hadi H. Khaligh, Irene A. Goldthorpe, Shawn D. Wettig, Michael A. Pope
Article
Pharmacology & Pharmacy
Mohamed Aborig, Paul R. V. Malik, Shruti Nambiar, Pierre Chelle, Johnson Darko, Anthony Mutsaers, Andrea N. Edginton, Andre Fleck, Ernest Osei, Shawn Wettig
Article
Pharmacology & Pharmacy
Jiahao Huang, Peter X. Chen, Michael A. Rogers, Shawn D. Wettig
Article
Chemistry, Applied
Shannon P. Callender, Shawn D. Wettig
Summary: Microemulsion systems have gained significant interest in pharmaceutical applications, with non-ionic surfactants being preferred for their uncharged nature and safety profile. The study analyzed the phase behavior and microemulsion formation of four non-ionic surfactants, revealing differences in behavior despite similar hydrophilic-lipophilic balance values. Surfactants like Polysorbate 80 and PEG-40 hydrogenated castor oil showed high synergism and potential for various applications.
JOURNAL OF SURFACTANTS AND DETERGENTS
(2021)
Review
Pharmacology & Pharmacy
Ahsan Ayub, Shawn Wettig
Summary: Drug delivery to the brain is a challenging task due to the blood-brain barrier. Nanomedicine, which combines nanotechnology, chemistry, and medicine, has shown promising results in improving drug delivery to the brain. Inorganic and organic nanoparticulate systems are being studied for this purpose.
Article
Chemistry, Physical
Robert D. E. Henderson, Carina T. Filice, Shawn Wettig, Zoya Leonenko
Summary: This study provides direct evidence of electrostatic interactions between gemini surfactant molecules and DNA strands on a cellular level, visualized using KPFM and correlated with their topography from AFM. The difference in topography and electrical surface potential between monolayers with and without DNA is significant, with strongly positive relative electrical surface potential observed in between lipid domains and DNA strands. These results suggest that cationic surfactant molecules likely surround DNA strands within a sea of background lipids.
Article
Chemistry, Physical
S. M. Shortall, D. G. Marangoni, S. D. Wettig
PHYSICAL CHEMISTRY CHEMICAL PHYSICS
(2020)
Article
Chemistry, Multidisciplinary
Aleisha McLachlan, Kulbir Singh, Michael McAlduff, D. Gerrard Marangoni, Samantha Shortall, Shawn D. Wettig