Review
Pharmacology & Pharmacy
Deepak Kulkarni, Fouad Damiri, Satish Rojekar, Mehrukh Zehravi, Sarker Ramproshad, Dipali Dhoke, Shubham Musale, Ashiya A. Mulani, Pranav Modak, Roshani Paradhi, Jyotsna Vitore, Md Habibur Rahman, Mohammed Berrada, Prabhanjan S. Giram, Simona Cavalu
Summary: Microneedle (MNs) technology is a recent advancement in biomedical science that has gained popularity worldwide due to its multifaceted and broad-spectrum applications in drug delivery. The limitations of conventional drug delivery, such as poor absorption and bioavailability, can be overcome by MN-based drug delivery. Nanotechnology has played a significant role in the fabrication techniques and design of microneedles.
Article
Biotechnology & Applied Microbiology
Kunal S. Parikh, Revaz Omiadze, Aditya Josyula, Richard Shi, Nicole M. Anders, Ping He, Youseph Yazdi, Peter J. McDonnell, Laura M. Ensign, Justin Hanes
Summary: Sutures are commonly used to modulate local, postoperative biological responses and prevent bacterial infections. Loading drugs directly into nanofiber-based sutures allows sustained drug delivery while meeting size and strength requirements for microsurgical ocular procedures.
BIOENGINEERING & TRANSLATIONAL MEDICINE
(2021)
Article
Chemistry, Physical
Beibei Lu, Tianqi Liu, Hao Wang, Chengyu Wu, Hanjun Chen, Zhe Liu, Jiaheng Zhang
Summary: Transdermal drug delivery system has several advantages, and ionic liquids play an important role in transdermal drug delivery.
JOURNAL OF MOLECULAR LIQUIDS
(2022)
Article
Pharmacology & Pharmacy
Kristyna Dvorakova, Petr Stepanek, Jirina Kroupova, Jarmila Zbytovska
Summary: Transdermal drug delivery is a non-invasive method with advantages over conventional routes of administration. However, the skin barrier needs to be modulated with enhancers, and currently there is a lack of enhancers with low toxicity and reversible effects. A study found that a series of new N-alkylmorpholines showed enhanced transdermal and dermal delivery, with the most effective derivatives having 10-14 carbons. The enhancers interacted predominantly with stratum corneum lipids.
Review
Pharmacology & Pharmacy
Ayah Mohammad Burhan, Butsabarat Klahan, Wayne Cummins, Vanessa Andres-Guerrero, Mark E. Byrne, Niall J. O'Reilly, Anuj Chauhan, Laurence Fitzhenry, Helen Hughes
Summary: This study presents an overview of posterior segment eye diseases, barriers to topical drug delivery, and the application of chitosan in ophthalmic drug delivery. It discusses how mucoadhesive formulations can help enhance drug delivery to the posterior eye segment.
Review
Pharmacology & Pharmacy
Kanokwan Singpanna, Chaiyakarn Pornpitchanarong, Prasopchai Patrojanasophon, Theerasak Rojanarata, Tanasait Ngawhirunpat, S. Kevin Li, Praneet Opanasopit
Summary: Transdermal drug delivery via the skin is a promising method, and gold nanoparticles (AuNPs) have emerged as a useful tool in this area. This review provides a comprehensive summary of the properties, synthesis, and applications of AuNPs in transdermal drug delivery.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Y. Han, Z. Y. Jin, D. S. Zhang, B. B. Hu, Z. Q. Li, Y. S. Jing, S. G. Sun
Summary: The transdermal drug delivery system (TDDS) can increase patient compliance, but many drugs are not easily absorbed through the skin due to the barrier function. Polymers can promote transdermal absorption as a chemical penetration promoter or as a raw material, and this article introduces the structure and mechanism of the skin, as well as the classification of polymers.
MATERIALS TODAY CHEMISTRY
(2022)
Article
Nanoscience & Nanotechnology
Rahman Md Moshikur, Islam Md Shimul, Shihab Uddin, Rie Wakabayashi, Muhammad Moniruzzaman, Masahiro Goto
Summary: In this study, we synthesized 12 oil-miscible ionic liquid drugs and found that one formulation containing oleate had 2.6 times higher permeation ability than the traditional levamisole salt. Animal experiments showed that the levamisole ionic liquid had higher plasma concentration and longer elimination half-life compared to the levamisole salt. Additionally, the levamisole ionic liquid demonstrated excellent biocompatibility. Therefore, oil-miscible ionic liquid drugs provide a simple and scalable strategy for the design of effective transdermal drug delivery systems.
ACS APPLIED MATERIALS & INTERFACES
(2022)
Article
Chemistry, Multidisciplinary
Tae Hyeon Kim, Na Yeon Kim, Hee Uk Lee, Ji Wook Choi, Taewook Kang, Bong Geun Chung
Summary: Cancer is a leading cause of death worldwide, and conventional cancer therapy has limitations. To address these issues, a transdermal drug delivery system based on iontophoresis has been developed. Controlled by a smartphone application, this system significantly enhances drug permeation at the tumor site and reduces systemic side effects.
JOURNAL OF CONTROLLED RELEASE
(2023)
Article
Pharmacology & Pharmacy
Anna-Lena Elksnat, Paula Zscherpe, Karina Klein, Jessika Maximiliane Cavalleri, Jessica Meissner
Summary: The study demonstrates that the use of an oxygen-based medical device can enhance the permeation of drugs, particularly for drugs with lower molecular weight.
Article
Pharmacology & Pharmacy
Mengzhen Xing, Yuning Ma, Xiaocen Wei, Chen Chen, Xueli Peng, Yuxia Ma, Bingwen Liang, Yunhua Gao, Jibiao Wu
Summary: Auxiliary permeable microneedles (AP-MNs) were prepared using polyvinyl alcohol and Eudragit NM30D to enhance transdermal drug delivery. The formulation of AP-MNs was optimized based on swelling properties, skin insertion, solution viscosity, and needle integrity. The AP-MNs exhibited excellent mechanical strength and hydrogel-forming properties, creating a continuous and unblockable network channel. The cumulative permeation of acidic and alkaline model drugs, azelaic acid and matrine, significantly increased after using AP-MNs.
Article
Medicine, General & Internal
Tory R. Spindle, Dennis J. Sholler, Edward J. Cone, Timothy P. Murphy, Mahmoud ElSohly, Ruth E. Winecker, Ronald R. Flegel, Marcel O. Bonn-Miller, Ryan Vandrey
Summary: This study evaluated the accuracy of CBD and THC labeling in topical cannabinoid products and found that they are often inaccurately labeled and many contain THC. These findings suggest the need for clinical studies to determine whether topical cannabinoid products with THC can produce psychoactive effects or positive drug tests for cannabis.
Article
Biochemistry & Molecular Biology
Janonna Kadyrov, Lanie Ruiz-Perez, Heather A. E. Benson, Ricardo L. Mancera
Summary: This study uses molecular dynamics simulations to investigate the mechanism of prodrugs' permeation through the skin, and finds that increased hydrophobicity can enhance drug permeation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Jiawei Ling, Yanan Du, Yuze Sheng, Weiqin Wang, Hangyi Wu, Guorong Chen, Huixia Lv
Summary: In vitro permeation test (IVPT) is commonly used for evaluating topical preparations and transdermal drug delivery systems. However, the storage of ex vivo skin for IVPT is challenging. This study investigated the efficacy of two cryopreservation media, 10% DMSO and 10% GLY, for preserving rat and pig skin at -20°C and -80°C, and found that -80°C storage in 10% DMSO or 10% GLY was optimal for maintaining skin viability and permeability. The results also suggested that skin viability could serve as a potential indicator for IVPT skin.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2023)
Article
Chemistry, Multidisciplinary
Ahlam Zaid Alkilani, Rania Hamed, Hajer Abdo, Lubna Swellmeen, Haneen A. Basheer, Walaa Wahdan, Amani D. Abu Kwiak
Summary: This study investigates the use of niosomes, a type of nanocarrier, to enhance the transdermal permeability of azithromycin, a BCS class III drug. The results show that niosomal gel can significantly improve the drug release rate compared to conventional gel formulations. These findings suggest that niosomal gel could be a promising alternative route of administration for azithromycin.
Article
Pharmacology & Pharmacy
Yutaka Inoue, Mari Shigematsu, Takanori Komatsu, Toshio Oguchi, Florencio Arce, Gerard Lee See
Summary: In this study, Rifampicin solutions were prepared using beta-cyclodextrin and gamma-cyclodextrin, and their spectroscopic properties and solubility were characterized. The results showed that Rifampicin formed complexes with both beta-cyclodextrin and gamma-cyclodextrin, and the different inclusion patterns led to an increase in solubility.
Article
Pharmacology & Pharmacy
Naoto Ono, Tomoya Iibuchi, Hiroaki Todo, Shoko Itakura, Hirotoshi Adachi, Kenji Sugibayashi
Summary: Thermalporation is an effective method for improving skin permeation of middle and high molecular weight biopharmaceuticals. The study showed that using the PassPort(R) system can significantly enhance the skin permeation of FD-4 and insulin, with improved relative bioavailability of insulin. Additionally, the skin resistance value decreased immediately after the PS treatment but returned to the initial level within 12 hours.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Akie Okada, Rina Niki, Yutaka Inoue, Junki Tomita, Hiroaki Todo, Shoko Itakura, Kenji Sugibayashi
Summary: In recent years, the development of self-injectable formulations has gained significant attention. In this study, a lipid-based depot formulation containing a easily metabolizable drug was prepared using a novel non-lamellar liquid-crystal-forming lipid. The results showed that the MGE-containing formulations had a micellar structure and improved the bioavailability and stability of the drug. This is of great importance for the development of self-administered peptide drugs and easily metabolized nucleic acids.
Article
Pharmacology & Pharmacy
Ryoki Kunita, Takafumi Nishijima, Hiroaki Todo, Kenji Sugibayashi, Hitoshi Sakaguchi
Summary: A novel mathematical model was established in this study, considering the permeation parameters and water evaporation, to evaluate the potential application of parameters obtained from artificial membrane Strat-M(R) in the safety assessment of cosmetic and dermopharmaceutical products.
Review
Pharmacology & Pharmacy
Kenji Sugibayashi
Summary: This article discusses the analytical methods for percutaneous absorption and skin permeation of chemical substances, as well as the transdermal drug delivery system (TDDS) that has been researched for about half a century. It first introduces the skin structure and definitions of scientific terms, then describes the experimental methods established for studying the percutaneous absorption and skin permeation of chemical substances, and finally outlines the analytical methods for the percutaneous absorption rate.
YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN
(2022)
Article
Chemistry, Multidisciplinary
Kenji Mori, Kotomi Yamazaki, Chihiro Takei, Takeshi Oshizaka, Issei Takeuchi, Kunio Miyaji, Hiroaki Todo, Shoko Itakura, Kenji Sugibayashi
Summary: A prototyped remote-controllable dosage management system was developed, allowing patients and caregivers to administer drugs via an internet line without touching the dosage device. The system consists of a transmitter located away from the patient and a dosage device equipped with a receiver, dosage management unit, and a drug treatment unit. In this study, the system was applied to in vitro permeation of a model drug, demonstrating successful remote-controlled drug administration.
JOURNAL OF CONTROLLED RELEASE
(2023)
Article
Chemistry, Multidisciplinary
Takeshi Oshizaka, Mao Hayakawa, Mayu Uesaka, Kota Yoshizawa, Tomoyo Kamei, Issei Takeuchi, Kenji Mori, Shoko Itakura, Hiroaki Todo, Kenji Sugibayashi
Summary: In this study, an ionic liquid-type enhancer IL-Azone was designed and found to have moderate enhancing effects on skin permeation. Although its enhancing effect was not as high as Azone, IL-Azone still showed potential as a skin penetration enhancer.
PHARMACEUTICAL RESEARCH
(2023)
Article
Chemistry, Multidisciplinary
Mika Futaki, Kazuya Inamura, Miyu Hashimoto, Shunsaku Motegi, Shoko Itakura, Kenji Sugibayashi, Hiroaki Todo
Summary: In this study, the effect of administration volume on drug distribution and pharmacokinetics parameters after intradermal injection using hollow microneedles (hMNs) was investigated. The results showed that drug distribution in the skin is related to pharmacokinetics parameters, and the number of needles and administration volume should be considered when designing hMN systems.
PHARMACEUTICAL RESEARCH
(2023)
Article
Multidisciplinary Sciences
Shoko Itakura, Ayaka Shohji, Sayaka Amagai, Masashi Kitamura, Kozo Takayama, Kenji Sugibayashi, Hiroaki Todo
Summary: In this study, siRNAs were loaded into grapefruit-derived extracellular vesicles (GEVs) using a microfluidic device (MD), resulting in the formation of GEVs-siRNA-GEVs. The morphology of GEVs and siRNA-GEVs was observed using cryogenic transmission electron microscopy, and the cellular uptake and intracellular trafficking of these vesicles were evaluated in human keratinocytes. The study demonstrates the potential of MDs for the preparation of siRNA-loaded EV formulations.
SCIENTIFIC REPORTS
(2023)
Article
Engineering, Chemical
Yutaka Inoue, Ayumi Nanri, Florencio Arce, Gerard Lee See, Takashi Tanikawa, Takami Yokogawa, Masashi Kitamura
Summary: A three-component inclusion complex of ascorbyl palmitate (ASCP), urea (UR), and gamma-cyclodextrin (gamma CD) with a molar ratio of 1/12 has been prepared using the evaporation method and the grinding and mixing method. The physical and chemical properties of the complexes were investigated, and it was found that the grinding and mixing method induced new diffraction peaks and phase transition of urea. The complex formed by the grinding and mixing method at a molar ratio of 1/2 showed inclusion complexes of gamma CD.
Review
Chemistry, Medicinal
Kozo Takayama, Shoko Itakura, Hiroaki Todo, Kenji Sugibayashi
Summary: Various stresses and strains are generated on the surface and inside of pharmaceutical tablets when an external force is applied. Numerical simulation using finite element method (FEM) is applied to measure stress and strain generation as experimental methods are difficult. The Drucker-Prager cap (DPC) model is recognized for representing stress distributions during compaction of powder to tablet form.
CHEMICAL & PHARMACEUTICAL BULLETIN
(2023)
Article
Chemistry, Medicinal
Takeshi Oshizaka, Rena Inaba, Mana Isono, Chihiro Takei, Issei Takeuchi, Kenji Mori, Kenji Sugibayashi
Summary: This study investigated the impact of the polarity of constituent cations in ionic liquids on membrane permeation, and found that the membrane permeability of ILs is not affected by the Ko/w of the constituent p-alkylbenzoic acid. The results suggest that the resulting IL does not affect membrane permeability even when the Ko/w of IL constituents markedly differs.
CHEMICAL & PHARMACEUTICAL BULLETIN
(2022)
Review
Biochemistry & Molecular Biology
Lord Sam Liston, Precious Lorraine Rivas, Pajaree Sakdiset, Gerard Lee See, Florencio Arce Jr
Summary: This paper reports on the permeation-enhancing properties and safety of different chemical permeation enhancers (CPEs) on the topical delivery of vitamin C (VC) and its derivatives. The majority of the CPEs belonged to low toxicity hazard category, and the combination of isopropyl myristate, sorbitan monolaurate, and polyoxyethylene 80 showed the highest permeation enhancement ratio for VC.
Article
Chemistry, Medicinal
Natsumi Hashimoto, Shigeru Tatsuta, Hisashi Kitamura, Misa Katsuyama, Kentaro Uchida, Kenji Sugibayashi
Summary: This study compared the effects of iontophoresis and electroporation on the penetration of sodium hyaluronate into the skin, and found that the combination of electroporation and iontophoresis increased the penetration of sodium hyaluronate with higher molecular weight into the stratum corneum, and there was a positive correlation between the penetration amount and the molecular weight.
CHEMICAL & PHARMACEUTICAL BULLETIN
(2022)
Article
Chemistry, Medicinal
Chihiro Takei, Kenji Mori, Takeshi Oshizaka, Kenji Sugibayashi
Summary: Ferrofluids are colloidal liquids that can change shape according to external magnetic field. In this study, magnetic field-responsive release of a model drug was observed using a depot-type injection containing white petrolatum and/or hydrophilic cream with a magnetic fluid. The concentration of the magnetic fluid affected the release, and a greater magnetic field-responsive release was observed with a combination of white petrolatum and hydrophilic cream.
CHEMICAL & PHARMACEUTICAL BULLETIN
(2022)
Article
Pharmacology & Pharmacy
Greta Camilla Magnano, Marika Quadri, Elisabetta Palazzo, Roberta Lotti, Francesca Loschi, Stefano Dall'Acqua, Michela Abrami, Francesca Larese Filon, Alessandra Marconi, Dritan Hasa
Summary: This study aimed to investigate the loading of sildenafil citrate in three commercial transdermal vehicles using 3D full-thickness skin equivalent and compare the results with permeability experiments using porcine skin. The results showed that the results obtained using the 3D skin equivalent were comparable to those obtained using porcine skin, suggesting that the 3D skin model can be a valid alternative for ex-vivo skin absorption experiments.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2024)
Article
Pharmacology & Pharmacy
James W. Mckeage, Andrew Z. H. Tan, Andrew J. Taberner
Summary: Needle-free jet injection is a promising alternative drug delivery technique that offers rapid, non-invasive, and large-volume injections. The study presents a prototype multi-orifice nozzle and a computational fluid dynamic model to demonstrate the feasibility and effectiveness of this technology.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2024)