Article
Pharmacology & Pharmacy
Hussam Murad, Osama Ahmed, Thamer Alqurashi, Mostafa Hussien
Summary: The self-microemulsifying drug delivery system of olmesartan medoxomil (OMS) was found to have better anti-inflammatory, antioxidant, and anti-apoptotic effects in TNBS-induced acute colitis in rats compared to olmesartan medoxomil alone.
Article
Pharmacology & Pharmacy
Sarwar Beg, Imran Kazmi, Obaid Afzal, Abdulmalik Saleh Alfawaz Altamimi, Fahad A. Al-Abbasi, Waleed H. Almalki, Saad Alghamdi, Majed Alrobaian, Khalid S. Alharbi, Mohammed S. Alshammari, Sunil K. Panda, Ibrahim Abdel Aziz Ibrahim, Tanuja Singh, Mahfoozur Rahman
Summary: The study systematically developed a phospholipid-based nanomixed micellar formulation of olmesartan medoxomil, surface-decorated with bile salt, to enhance lymphatic drug targeting and systemic availability. In vitro and in vivo experiments demonstrated the formulation's sustained drug release, high cellular uptake, and significant improvements in pharmacokinetics and lymphatic uptake compared to a pure drug suspension.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2021)
Article
Pharmacology & Pharmacy
Yelda Komesli, Yeliz Yildirim, Ercument Karasulu
Summary: The biodistribution of hydrophobic olmesartan medoxomil self-microemulsifying drug delivery system (OM-SMEDDS) was successfully visualized using fluorescent dyes in this study, showing significantly stronger emission than the control group. Ex-vivo organ imaging further confirmed the enhanced fluorescence emission for OM-SMEDDS compared to controls.
DRUG METABOLISM AND PHARMACOKINETICS
(2021)
Article
Pharmacology & Pharmacy
Yong-Han Kim, Seong-Bo Kim, Se-Hee Choi, Thi-Thao-Linh Nguyen, Sung-Hoon Ahn, Kyung-Sun Moon, Kwan-Hyung Cho, Tae-Yong Sim, Eun-Ji Heo, Sung Tae Kim, Hyun-Suk Jung, Jun-Pil Jee, Han-Gon Choi, Dong-Jin Jang
Summary: The purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble olaparib. The study focused on selecting pharmaceutical excipients and identifying self-emulsifying regions. Various physicochemical properties of the microemulsion incorporating olaparib were investigated, and its improved dissolution and absorption were confirmed. The optimal microemulsion formulation was generated using specific ingredients, and it exhibited good dispersion and stability.
Article
Biology
Weiyin Huang, Shuang Chen, Lin Sun, Hubin Wwang, Hongqun Qiao
Summary: The study investigated the intestinal permeability of lamivudine using Caco-2 cells monolayer and single-pass intestinal perfusion, revealing a passive diffusion absorption mechanism possibly related to efflux transporters. Lamivudine was classified as a moderate-permeability drug in the Biopharmaceutics Classification System.
SAUDI JOURNAL OF BIOLOGICAL SCIENCES
(2022)
Article
Chemistry, Medicinal
Ling Lin, Sajid Asghar, Lin Huang, Ziyi Hu, Qineng Ping, Zhipeng Chen, Feng Shao, Yanyu Xiao
Summary: The study aimed to enhance the water solubility and oral bioavailability of Chl through a self-microemulsifying drug delivery system (Chl-SMEDDS). The optimized formulation showed stable physical characteristics and improved drug dispersion, with the main absorption site in the duodenum, suggesting that SMEDDS could be an effective strategy for Chl oral administration.
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
(2021)
Review
Chemistry, Medicinal
Maisarah Azman, Akmal H. Sabri, Qonita Kurnia Anjani, Mohd Faiz Mustaffa, Khuriah Abdul Hamid
Summary: The oral route is the most common and practical means of drug administration. However, drug absorption through the intestinal wall is influenced by various factors, including the presence of efflux transporters, enzymatic degradation, and tight junctions. Hydrophilic drugs, high molecular weight drugs, and efflux transporter substrates face more challenges in terms of absorption. Another challenge is first-pass hepatic metabolism, which can reduce drug bioavailability. Various compounds have been studied for their permeation-enhancing effects, and nanocarrier-based formulations have also gained interest in enhancing oral drug absorption.
Review
Pharmacology & Pharmacy
Alessandra T. Zizzari, Dimanthi Pliatsika, Flavio M. Gall, Thomas Fischer, Rainer Riedl
Summary: Peptides, due to their structural diversity, are considered a unique source of innovative active ingredients, but face challenges in development due to their disadvantageous pharmacokinetic properties. Recent efforts have focused on improving the oral bioavailability of peptide drugs, with the latest findings expected to influence future approaches in developing more efficient and safer orally delivered peptides by pharmaceutical companies.
DRUG DISCOVERY TODAY
(2021)
Review
Pharmacology & Pharmacy
Zichen Zhang, Yi Lu, Jianping Qi, Wei Wu
Summary: Orally administered drugs must survive the gastrointestinal environment, penetrate the enteric epithelia, and avoid hepatic metabolism before reaching the systemic circulation. Hepatic metabolism is a significant barrier, and alternative pathways like intestinal lymphatic transport are being explored. Main pathways for peroral lymphatic transport include the chylomicron and microfold cell pathways, with increasing research input and applications.
ACTA PHARMACEUTICA SINICA B
(2021)
Article
Spectroscopy
Amira H. Kamal, Sherin F. Hammad, Doaa N. Kamel
Summary: Four UV chemometric spectrophotometric techniques were developed and tested for determination of AML and OLM, achieving linearity in the concentration range of 2-25 μg/mL. The methods were found to be uncomplicated, reproducible, efficient, and cost-effective for determining the drugs in laboratory samples and commercial pharmaceutical formulations.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2022)
Article
Instruments & Instrumentation
Annalisa Rosso, Eyad Almouazen, Jorge Pontes, Valentina Andretto, Marine Leroux, Etienne Romasko, Samira Azzouz-Maache, Claire Bordes, Isabelle Coste, Touffic Renno, Stephane Giraud, Stephanie Briancon, Giovanna Lollo
Summary: This study explored the design of supersaturable self-microemulsifying drug delivery systems (S-SMEDDS) to improve oral absorption of a novel benzimidazole derivative anticancer drug (BI) with poor solubility. The results showed that the supersaturable systems promoted drug absorption in vivo compared to conventional formulations, highlighting their potential as an alternative for enhancing oral systemic absorption of lipophilic drugs.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2021)
Article
Plant Sciences
Patcharawalai Jaisamut, Subhaphorn Wanna, Surasak Limsuwan, Sasitorn Chusri, Kamonthip Wiwattanawongsa, Ruedeekorn Wiwattanapatapee
Summary: The study proposed a drug delivery system to enhance the oral bioavailability of quercetin and resveratrol. The self-microemulsifying formulation significantly improved the oral bioavailability of the combined compounds, without compromising their biological activities, showing promising potential for future research.
Article
Materials Science, Biomaterials
Jyotsana R. Madan, Kajal Patil, Rajendra Awasthi, Kamal Dua
Summary: This study successfully developed a solid self-microemulsifying drug delivery system (S-SMEDDS) to enhance the solubility of azilsartan medoxomil. The system demonstrated good flow property, spontaneous self-microemulsification property, and improved in vitro dissolution profile compared to pure azilsartan medoxomil.
INTERNATIONAL JOURNAL OF POLYMERIC MATERIALS AND POLYMERIC BIOMATERIALS
(2021)
Review
Pharmacology & Pharmacy
Carlynne Choy, Lee Yong Lim, Lai Wah Chan, Zhixiang Cui, Shirui Mao, Tin Wui Wong
Summary: This review examines the potential of targeting intestinal receptors to improve the oral delivery of nanoinsulin. While promising, further research and optimization are needed.
PHARMACOLOGICAL REVIEWS
(2022)
Article
Pharmacology & Pharmacy
Katherine C. Fein, John P. Gleeson, Alexandra N. Newby, Kathryn A. Whitehead
Summary: Decades of research on oral peptide drugs have led to clinically successful formulations, often utilizing permeation enhancers to facilitate absorption in the intestines. This study examined the effects of two permeation enhancers on the transport of macromolecules of varying sizes, highlighting their potential to improve the absorption of proteins.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2022)