Article
Chemistry, Multidisciplinary
Moritz Radbruch, Hannah Pischon, Fang Du, Rainer Haag, Fabian Schumacher, Burkhard Kleuser, Lars Mundhenk, Achim D. Gruber
Summary: The polymeric core-multishell nanocarrier (CMS) shows promise as a carrier for topical delivery of tacrolimus (TAC). However, in vivo, it does not increase TAC penetration into the skin compared to ointment. Nevertheless, the therapeutic efficacy of TAC delivered by CMS is equivalent to standard TAC ointment.
JOURNAL OF CONTROLLED RELEASE
(2022)
Article
Pharmacology & Pharmacy
Kevin McLean, Wenbo Zhan
Summary: Nanoparticle-mediated topical delivery has the potential to significantly improve drug exposure in deep skin tissue. Adequate and long-term drug-skin contact is important for effective drug deposition. The release rate of nanoparticles should be controlled to achieve optimal drug accumulation in different skin layers.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Pharmacology & Pharmacy
Ines Nikolic, Mitar Simic, Ivana Pantelic, Goran Stojanovic, Jelena Antic Stankovic, Bojan Markovic, Snezana Savic
Summary: Various approaches have been proposed for improving dermal drug delivery, such as chemical penetration enhancers and electrical current methods like iontophoresis. In this study, curcumin-loaded nanoemulsions with and without monoterpenes as penetration enhancers, as well as an adhesive dermal delivery system based on iontophoresis, were designed and evaluated. The results showed that iontophoresis was equally efficient as other methods in terms of curcumin penetration through superficial skin layers. Further improvement of iontophoresis as a mobile adhesive system would be a practical contribution in the field of dermal drug application.
Review
Pharmacology & Pharmacy
Danielle van Staden, Richard K. K. Haynes, Joe M. M. Viljoen
Summary: Self-emulsification is a formulation technique that improves oral drug delivery by enhancing solubility and bioavailability. It provides a simplified method for delivering lipophilic drugs by producing emulsions upon moderate agitation and dilution. It is also a promising approach for topical drug delivery, offering simplified production procedures and unlimited upscaling possibilities.
Review
Chemistry, Multidisciplinary
Lingbo Shen, Guihua Fang, Bo Tang, Qiang Zhu
Summary: Topical corticosteroids are the primary treatment for ocular inflammation, and factors such as drug properties and administration strategies affect drug bioavailability in the eye. Currently, there is a lack of rational and dynamic approaches to strategy selection.
JOURNAL OF CONTROLLED RELEASE
(2021)
Article
Instruments & Instrumentation
Chin-Ping Kung, Bruno C. Sil, Yanling Zhang, Jonathan Hadgraft, Majella E. Lane, Bhumik Patel, Renee McCulloch
Summary: Amitriptyline, currently used for neuropathic pain and migraine, is being explored as a potential topical analgesic. Initial studies suggest that formulations containing isopropyl myristate (IPM) and isopropyl alcohol (IPA) promote higher permeation of amitriptyline through the skin, while those containing propylene glycol (PG) also show promise for dermal delivery. Further optimization is needed for clinical investigational studies.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2022)
Article
Pharmacology & Pharmacy
Jamal Alyoussef Alkrad, Reinhard H. H. Neubert
Summary: In this study, insulin was successfully loaded into nano-sized non-ionic colloidal carrier systems for transdermal drug delivery. The CCS exhibited excellent rheological properties and drug release rate. The insulin-loaded CCS showed high transdermal flux through rat's skin and epidermis, and induced a delayed therapeutic effect.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Review
Nanoscience & Nanotechnology
Lin Sun, Hong Xiang, Canfeng Ge, Xingxu Chen, Qian Zhang, Yanzhuo Zhang, Xiaoqing Miao
Summary: Nanocrystals, with their high stability and sustained drug release profiles, offer an efficient method for topical drug delivery. The success of drug nanocrystals in skin disease therapy relies heavily on previous skin treatments, choice of excipients and penetration enhancement strategies.
JOURNAL OF BIOMEDICAL NANOTECHNOLOGY
(2021)
Article
Dermatology
Soraya Babaie, Mohammad Charkhpour, Maryam Kouhsoltani, Hamed Hamishehkar, Ana Claudia Paiva-Santos
Summary: By using lipid-based nanovesicles, buprenorphine and bupivacaine can be co-delivered to effectively target pain receptors concentrated in the skin, resulting in potent dermal anesthesia.
EXPERIMENTAL DERMATOLOGY
(2023)
Review
Pharmacology & Pharmacy
Supreeda Tambunlertchai, Sean M. Geary, Aliasger K. Salem
Summary: Malignant melanoma is a form of aggressive skin cancer with no reliable therapy available currently. Topical drug delivery is being explored as an alternative, but the stratum corneum poses a barrier to drug penetration, leading to research focusing on strategies to enhance skin penetration.
Article
Biochemistry & Molecular Biology
Alexandra Gruber, Aaroh Anand Joshi, Patrick Graff, Jose Luis Cuellar-Camacho, Sarah Hedtrich, Daniel Klinger
Summary: Polymeric nanogels are potential nonirritating nanocarriers for topical delivery. Amphiphilic nanogels containing hydrophilic networks with hydrophobic domains can overcome the limitations of conventional hydrophilic networks, improving encapsulation of hydrophobic therapeutics and tailored interactions with the skin barrier.
Article
Chemistry, Multidisciplinary
Anna Lena Klein, Markus Lubda, David Specht, Sung-Min Pyo, Loris Busch, Juergen Lademann, Martina C. Meinke, Ingeborg Beckers, Joerg von Hagen, Cornelia M. Keck, Alexa Patzelt
Summary: This study utilized dermal microdialysis on ex vivo porcine ear skin to investigate penetration kinetics of caffeine, revealing differences in penetration effects between different sizes and types of caffeine nanocrystals, and confirming the validity of microdialysis data.
Article
Engineering, Environmental
Wei Gao, Yongfeng Lin, Yong Liang, Yingjun Wang, Lu Jiang, Yawei Wang, Guibin Jiang
Summary: The experiment revealed that the penetration ability of CPs through the skin was correlated with their molecular structure, with short-chain and medium-chain CPs more easily penetrating the skin compared to long-chain CPs. Additionally, the study suggests that human dermal exposure to CPs could be a significant pathway for CPs intake in the environment, highlighting the importance of further research in this area.
JOURNAL OF HAZARDOUS MATERIALS
(2021)
Article
Pharmacology & Pharmacy
Thirapit Subongkot, Tanasait Ngawhirunpat, Praneet Opanasopit
Summary: This study aimed to develop ultradeformable liposomes with fatty acids to improve the skin penetration of rosmarinic acid, and found that ULs with oleic acid significantly increased the skin penetration of rosmarinic acid via the transfollicular pathway. Confocal laser scanning microscopy observations showed that UL vesicles attach to the skin before releasing the entrapped drug to penetrate the skin.
Article
Chemistry, Analytical
Shahrukh Zaman Akash, Farjana Yesmin Lucky, Murad Hossain, Asim Kumar Bepari, G. M. Sayedur Rahman, Hasan Mahmud Reza, Shazid Md Sharker
Summary: The development of externally controlled drug delivery systems that can rapidly trigger drug release is expected to change the landscape of future drug carriers. A temperature-responsive paraffin film was developed for on-demand drug release and therapeutic effects, providing flexible control of dose magnitude and timing. These remotely adjustable drug delivery systems can significantly improve patient compliance and medical practice through minimization of inflammation and microbial infection.
Article
Toxicology
Lekaashree Rambabu, Fahim Mohamed, Jeevan Dhanarisi, Indika Gawarammana, Jacques Raubenheimer, Lorraine Mackenzie, Michael S. Roberts, Nicholas Buckley, Michael Eddleston
Summary: Phethoate self-poisoning has a 6.5% case fatality rate. Most patients who experience respiratory failure undergo early intubation; most deaths occurred among those patients who were intubated less than 24 h after ingestion. There was a non-sustained increase in cholinesterase activity with pralidoxime, but further studies are required to analyse the extent to which oximes are clinically effective in phenthoate self-poisoning.
CLINICAL TOXICOLOGY
(2022)
Article
Critical Care Medicine
Maryam Hosseini, Michael S. Roberts, Reza Aboofazeli, Hamid R. Moghimi
Summary: This study characterized the affinity of human third-degree burn eschar for drugs by measuring Hansen Solubility Parameters (HSP). The results showed good correlations between solvent uptakes and HSP values, with the highest correlation observed for the bipolar parameter. Increased temperature decreased the HSP values, especially the hydrogen bonding parameter. Relative Energy Differences (RED) were found to be a good parameter for predicting drug-eschar affinity. These findings are important for drug selection and carrier design in drug delivery through burn eschar.
Article
Pharmacology & Pharmacy
Aymen A. Al-Qurain, Richard N. Upton, Rami Tadros, Michael S. Roberts, Michael D. Wiese
Summary: This study aimed to investigate the pharmacokinetic parameters of tramadol and its active metabolite in older patients and develop a population pharmacokinetic model. The results showed that tramadol exposure increased with frailty and reduced renal function. Therefore, prescribers should consider the frailty status and renal function to minimize the risk of tramadol toxicity in this population.
EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS
(2022)
Article
Chemistry, Multidisciplinary
Joshua J. Calcutt, Michael S. Roberts, Yuri G. Anissimov
Summary: This study develops a physiologically based pharmacokinetic and COMSOL based dermal transport model that considers the impact of the subpapillary dermal plexus on skin concentrations. Sensitivity analyses identify important factors that affect skin concentrations.
PHARMACEUTICAL RESEARCH
(2022)
Article
Chemistry, Multidisciplinary
Nathalie Jung, Sarika Namjoshi, Yousuf Mohammed, Jeffrey E. Grice, Heather A. E. Benson, Sam G. Raney, Michael S. Roberts, Maike Windbergs
Summary: This study presents the value of confocal Raman microscopy (CRM) as a tool for the evaluation of semisolid dosage forms in pharmaceutical research and development. CRM enables spatial analysis of microstructural features, drug distribution, and interaction with skin tissue.
PHARMACEUTICAL RESEARCH
(2022)
Article
Pharmacology & Pharmacy
Sean E. Mangion, Lydia Sandiford, Yousuf Mohammed, Michael S. Roberts, Amy M. Holmes
Summary: This study used multiphoton microscopy and fluorescence lifetime imaging microscopy to evaluate the delivery and dissolution of zinc pyrithione in hair follicles. The results showed that FLIM was the most suitable method for detection, with increased selectivity and sensitivity. The study found that zinc pyrithione particles could be detected up to 500 micrometers in aqueous suspensions.
Article
Multidisciplinary Sciences
Hanumanth Srikanth Cheruvu, Xin Liu, Jeffrey E. Grice, Michael S. Roberts
Summary: This article presents a dataset of maximal flux and permeability coefficient values obtained from In Vitro human skin Permeation Test (IVPT) reports. The dataset includes physicochemical properties of solutes and experimental conditions, as well as univariate Quantitative Structure-epidermal Permeability Relationships (QSPR). The data can be used for validating regression equations, predicting permeation parameters, and aiding in drug choice, product design, and characterizing skin exposure to hazardous substances.
Review
Pharmacology & Pharmacy
Yousuf Mohammed, Amy Holmes, Philip Chi Lip Kwok, Tushar Kumeria, Sarika Namjoshi, Mohammad Imran, Lana Matteucci, Masood Ali, Waiting Tai, Heather A. E. Benson, Michael S. Roberts
Summary: Epithelial surfaces play a crucial role in protecting the body from foreign materials and can be utilized for drug delivery. The permeability of different epithelia varies based on their exposure and function. Advancements in epithelial drug delivery systems have been driven by quality-by-design approach and the growth of generic products.
ADVANCED DRUG DELIVERY REVIEWS
(2022)
Article
Pharmacology & Pharmacy
Xin Liu, Hanumanth S. Cheruvu, Yuri G. Anissimov, John van der Hoek, Eleftheria Tsakalozou, Zhanglin Ni, Priyanka Ghosh, Jeffrey E. Grice, Michael S. Roberts
Summary: Pharmacokinetic models are widely used to describe drug permeation across the epidermal barrier. In this study, existing models were extended to describe drug concentrations, urinary excretion profiles, and exposure estimates after topical application. The models were validated and used to establish in vitro-in vivo relationships. Other study parameters can also impact drug permeability.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Pharmacology & Pharmacy
A. A. Amarah, J. Hadgraft, M. S. Roberts, Y. G. Anissimov
Summary: This work expands the compartmental model and improves the simulation of diffusion and partition within the stratum corneum, leading to significant improvement in fitting experimental data.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Chemistry, Medicinal
R. Marriott, T. I. Spiridonova, S. I. Tverdokhlebov, Y. G. Anissimov
Summary: Polymeric drug delivery systems can enhance patient compliance and therapeutic effects by controlling drug release, and mathematical models can facilitate their development. This study presents a new compartmental model that considers polymer degradation and drug diffusion to predict drug release, and applies the model to membranes, fibers, and particles of different geometries.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Chemistry, Analytical
Shuping Qiang, Fahim Mohamed, Lorraine Mackenzie, Michael S. Roberts
Summary: The potential exposure to glyphosate-based herbicides, including suicide attempts, is a global concern. The toxicokinetics of polyethoxylated tallow amine (POEA) surfactants after exposure is limited, due to the lack of suitable analysis methods. A robust LC-MSMS method was developed and validated for the rapid analysis of 11 POEA homologues in human plasma. The analysis of POEA surfactants plasma concentrations is crucial for assessing internal exposure and the relationships between glyphosate toxicity and poisoning extent.
Article
Chemistry, Medicinal
Afshin Zamani Zakaria, Owen G. Jepps, Tim Gould, Yuri G. Anissimov
Summary: Suitable numerical analysis of stratum corneum structure is essential to understand the diffusion mechanisms of percutaneous drug delivery. This research paper accounted for the permeable envelope layer in the finite element models and simulated penetration and desorption experiments using transient finite element analysis. The results showed that cornified lipid permeability (Penv) and lipid transverse diffusion coefficient (Dlip_trans) are important factors in desorption and penetration, respectively.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Krishna C. Telaprolu, Jeffrey E. Grice, Yousuf H. Mohammed, Michael S. Roberts
Summary: The distribution of esterase enzymes in different layers of human skin and their contributions to drug metabolism are poorly understood. In this study, methyl salicylate cream was tested on various human skin membranes to investigate esterase distribution. The results showed similar permeation of methyl salicylate across all membranes, suggesting dermal esterase activity. Staining studies also confirmed that esterase activity was mainly present in the dermal-epidermal junction region of the dermis rather than the epidermis.