Advances in Delivery of Irinotecan (CPT-11) Active Metabolite 7-Ethyl-10-Hydroxycamptothecin.

08:00 EDT 9th July 2019 | BioPortfolio

Summary of "Advances in Delivery of Irinotecan (CPT-11) Active Metabolite 7-Ethyl-10-Hydroxycamptothecin."

CPT-11 is a first-line chemotherapy for advanced or metastatic colorectal cancers (mCRC). SN38 (7-ethyl-10-hydroxycamptothecin), the active metabolite of CPT-11, has an anticancer efficacy 100-1000 folds more than CPT-11 in vitro. However, the drawbacks such as ultralow solubility and poor stability, greatly limit the clinical applications of SN38. Recently, SN38-based nanomedicines have greatly improved the pharmaceutical and therapeutic characteristics of SN38. In addition, these nanosized delivery systems can target tumor tissues via the EPR effect and/or active-targeting strategies, thereby significantly improving anticancer efficacy, reducing side effects and reversing drug resistance. This review focuses on the advances of nano-delivery systems for SN38. We categorize the published studies into two groups, physical encapsulation and chemical conjugation, for the development of SN38 nano-delivery systems, and particularly summarize those for active tumor targeting. The advantages and shortcomings of current SN38 nano-delivery systems, aiming to develop more potent SN38 nano-delivery systems, are also discussed.


Journal Details

This article was published in the following journal.

Name: International journal of pharmaceutics
ISSN: 1873-3476
Pages: 118499


DeepDyve research library

PubMed Articles [12573 Associated PubMed Articles listed on BioPortfolio]

Nanoparticulate delivery of irinotecan active metabolite (SN38) in murine colorectal carcinoma through conjugation to poly (2-ethyl 2-oxazoline)-b-poly (L-glutamic acid) double hydrophilic copolymer.

SN-38 is the active metabolite of irinotecan, an FDA-approved chemotherapeutic agent indicated for colorectal carcinoma, which would not be clinically applicable due to its very poorly soluble and hyd...

Mitochondria and nucleus delivery of active form of 10-hydroxycamptothecin with dual shell to precisely treat colorectal cancer.

The objective of this study was to deliver a ring-closed form of 10-hydroxycamptothecin (HCPT) to the mitochondria and nucleus to treat colorectal cancer.

A novel mechanism of irinotecan targeting MDM2 and Bcl-xL.

Irinotecan is a strong anticancer drug whose mechanism of action has been reported only for the inhibition of DNA topoisomerase I (Topo I) through its active metabolite SN-38. In this study, we presen...

Toward a better understanding of the mechanism of action for intra-arterial delivery of irinotecan from DC Bead (DEBIRI).

DC Bead is designed for the embolization of liver malignancies combined with local sustained chemotherapy delivery. It was first demonstrated around a decade ago that irinotecan could be loaded into D...

A UGT1A1 genotype-guided dosing study of modified FOLFIRINOX in previously untreated patients with advanced gastrointestinal malignancies.

FOLFIRINOX (5-fluorouracil [5-FU], leucovorin, irinotecan, oxaliplatin) is an effective but toxic therapy for pancreatic cancer. UGT1A1 (UDP glucuronosyltransferase 1A1) eliminates the active metaboli...

Clinical Trials [6596 Associated Clinical Trials listed on BioPortfolio]

Study of Glutamine as Prophylaxis for Irinotecan Induced Diarrhea

Irinotecan (7-ethyl-10- {4(-1-piperidino)-1-piperidino} carbonyloxy camptothecin) is a semisynthetic camptothecin derivative introduced in the 1980's. Irinotecan is a prodrug metabolized b...

Study to Evaluate the Pharmacokinetics of Telotristat Ethyl in Subjects With Severe Hepatic Impairment

This study is designed to evaluate the effect of severe hepatic impairment on the pharmacokinetics (PK) of telotristat ethyl (TE) ( LP-778902 active moiety, metabolite), following administ...

Mouthwash With Chlorhexidine 0.12%/Ethyl Alcohol 7% Compared to Ethyl Alcohol 7%

Clinical triple-blind randomized controlled trial to assess the use of two different mouthwashes to reduce the oral colonization by gramnegative bacteria in patients with chemotherapy indu...

BrUOG 329 GBM Onyvide With TMZ

New treatments are greatly needed for patients with recurrent glioblastoma. Metronomic temozolomide is a standard treatment option but has, at best, modest activity. The nanoliposomal irin...

fMRI of Hypothalamic Responses to Taste, Temperature and Glucose

The study will consist of five occasions with one week in between. BOLD signal intensity of the hypothalamus will be measured using fMRI. Measurements will be done before and after drinkin...

Medical and Biotech [MESH] Definitions

A gas that condenses under slight pressure. Because of its low boiling point ethyl chloride sprayed on skin produces an intense cold by evaporation. Cold blocks nerve conduction. Ethyl chloride has been used in surgery but is primarily used to relieve local pain in sports medicine.

9,10-Secoergosta-5,7,10(19),22-tetraene-3,25-diol. Biologically active metabolite of vitamin D2 which is more active in curing rickets than its parent. The compound is believed to attach to the same receptor as vitamin D2 and 25-hydroxyvitamin D3.

Organic compounds having ethyl groups bound to an oxygen atom

3-Ethyl-2-(5-(3-ethyl-2-benzothiazolinylidene)-1,3- pentadienyl)benzothiazolium. A benzothiazole that was formerly used as an antinematodal agent and is currently used as a fluorescent dye.

An anticonvulsant that is the active metabolite of TRIMETHADIONE.

Quick Search


DeepDyve research library

Relevant Topic

Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...

Searches Linking to this Article