Article
Pharmacology & Pharmacy
Rahman Md Moshikur, Md Korban Ali, Rie Wakabayashi, Muhammad Moniruzzaman, Masahiro Goto
Summary: This study transformed methotrexate (MTX) into a series of five ionic liquids to improve its oral bioavailability, with proline ethyl ester MTX (IL[ProEt][MTX]) showing the highest oral bioavailability in mice. IL[ProEt][MTX] had significantly higher plasma concentration, longer half-life, larger area under the plasma concentration, longer absorption time, and lower body clearance compared to MTX sodium, indicating improved in vivo absorption and reduced systemic toxicity. Mechanistic studies suggested that the spherical structures formed by IL[ProEt][MTX] solution contributed to its improved oral absorption performance. Antitumor studies also showed that IL[ProEt][MTX] had better tumor growth inhibition than MTX sodium.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Multidisciplinary Sciences
Yue Gao, Jingxue Nai, Zhenbo Yang, Jinbang Zhang, Siyu Ma, Yumei Zhao, Hui Li, Jiaxin Li, Yang Yang, Meiyan Yang, Yuli Wang, Wei Gong, Fanglin Yu, Chunsheng Gao, Zhiping Li, Xingguo Mei
Summary: The novel preparative method developed in this study successfully achieved high drug loading of nanoparticle albumin-bound (nab) paclitaxel by improving paclitaxel solubility in polyethylene glycol (PEG) and self-assembly into nanoparticles. The self-made nab paclitaxel showed similar characteristics to the commercial Abraxane in terms of morphology, in vitro release, and other analyses. This new method not only increases drug loading significantly, but also reduces production costs, showing significant practical value.
Article
Pharmacology & Pharmacy
Pavan K. Yadav, Ravi Saklani, Amrendra K. Tiwari, Saurabh Verma, Divya Chauhan, Pooja Yadav, a Rafquat Rana, Navodayam Kalleti, Jiaur R. Gayen, Srikanta K. Rath, Madhav N. Mugale, Kalyan Mitra, Manish K. Chourasia
Summary: This study co-encapsulated Paclitaxel and Baicalein in a nanoemulsion for breast cancer treatment. The optimized synergistic ratio was determined through cytotoxicity assessment, and the nanoemulsion was characterized using Quality by Design approach. The results showed that the nanoemulsion had significant anticancer effects in cell experiments and animal models, indicating its potential as a therapeutic approach for breast cancer.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Biochemistry & Molecular Biology
Alina Sesarman, Dana Muntean, Bianca Abrudan, Lucia Tefas, Bianca Sylvester, Emilia Licarete, Valentin Rauca, Lavinia Luput, Laura Patras, Manuela Banciu, Laurian Vlase, Alina Porfire
Summary: The study aimed to investigate the pharmacokinetic profile, tissue distribution, and adverse effects of long-circulating liposomes containing curcumin and doxorubicin. It demonstrated that the liposomal association of curcumin and doxorubicin effectively improved the pharmacokinetics and biodistribution of doxorubicin, limiting its side effects through curcumin-dependent antioxidant effects.
JOURNAL OF LIPOSOME RESEARCH
(2021)
Article
Pharmacology & Pharmacy
Chae Eun Jin, Moon Sup Yoon, Min Jeong Jo, Seo Yeon Kim, Jae Min Lee, Su Jeong Kang, Chun-Woong Park, Jin-Seok Kim, Dae Hwan Shin
Summary: Ovarian cancer has a high mortality rate due to difficult early detection, necessitating the development of a novel anti-cancer treatment with improved efficacy and reduced toxicity. Micelles encapsulating paclitaxel and sorafenib were prepared using the freeze-drying method, and the optimal polymer was selected based on various factors. The PTX/SRF micelles demonstrated slower release, improved bioavailability, and enhanced anticancer effects compared to single-drug therapy in ovarian cancer.
Article
Materials Science, Ceramics
Amrinder Singh, Shubham Thakur, Satwinderjeet Kaur, Subheet Kumar Jain
Summary: This study investigated the role of sodium bicarbonate in changing the hydrogen bonding within methyl cellulose to induce locoregional anticancer action of paclitaxel. The study found that the optimized thermosensitive in situ injectable nanovesicular formulation of paclitaxel showed better tumor control and reduced toxicity compared to the commercial formulation. The study also revealed that sodium bicarbonate successfully brought the gelation point of methyl cellulose below physiological temperature, imparting stiffness to the injectable formulation for localized effect.
JOURNAL OF SOL-GEL SCIENCE AND TECHNOLOGY
(2022)
Article
Chemistry, Organic
Lizeth Bodero, Sara Parente, Federico Arrigoni, Annika Klimpel, Ines Neundorf, Silvia Gazzola, Umberto Piarulli
Summary: Two new Drug Delivery Systems (DDS) containing the cyclo[DKP-isoDGR] integrin ligand and the cytotoxic agent Paclitaxel (PTX) were synthesized to investigate their influences on cellular uptake and cytotoxicity. Compound 3 showed significantly higher potency compared to compound 2, with reduced potency loss in comparison to PTX.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Integrative & Complementary Medicine
Dake Cai, Jing Jin, Huichang Bi, Guoping Zhong, Minhua Zhou, Jianfen Guo, Yike Cai, Miaoyin Liang, Qiong Gu, Zixuan Hu, Yijing Lai, Zi Dai, Lingjie Li, Yuxing Chen, Haili Gao, Min Huang
Summary: Taxus yunnanensis, a traditional Chinese herb for cancer treatment, contains paclitaxel and its extract shows good oral bioavailability. This study investigates the anti-tumor effect of the extract (HDS-1) through oral administration and explores the contribution of flavonoids (HDS-2) and lignoids (HDS-3) to its efficacy. The findings indicate that HDS-1 exerts significant inhibition on A549 tumor growth, while HDS-2 and HDS-3 enhance the absorption and cytotoxicity of paclitaxel, thus contributing to the anti-cancer effect of HDS-1.
EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
(2022)
Article
Pharmacology & Pharmacy
Kurawattimath Vishwanath, Barnabas Wilson, Kannoth Mukundan Geetha, Vedigounder Murugan
Summary: To treat glioma, researchers developed stable paclitaxel-loaded bovine serum albumin nanoparticles (BSA-NPs-PTX) as drug-delivery vehicles. BSA-NPs-PTX-Ps 80 showed higher plasma concentration-time curves and significantly improved PTX distribution in the frontal cortex, posterior brain, and cerebellum.
THERAPEUTIC DELIVERY
(2023)