Abstract：
:A new indole based chalcone molecule MOMIPP induced methuosis mediated cell death in gliobastoma and other cancer cell lines. But the drug was insoluble in water and had a very short plasma half-life. The purpose of this work was to develop a formulation that can provide sustained levels of MOMIPP in vivo. Initial studies established drug solubility in various solvents. N-methyl pyrrolidone (NMP) was determined as an excellent solvent for the drug. Subsequently a poloxamer-407 based thermoreversible gel containing NMP was used to develop the formulation. Rheological studies were performed via oscillatory temperature mode, continuous shear analysis, and oscillatory frequency mode experiments. The mechanical properties of the formulations were tested using a texture profile analyzer. The gelation temperature and time of formulations increased with increasing amounts of NMP. However, the viscosity at 20 °C and storage modulus decreased as the amount of NMP increased. Characterization studies helped to identify the gel formulation that was used to administer the drug orally, sub-cutaneously, and intra-peritoneally. When the gel was given intraperitoneally the target plasma and brain levels of over 5 μM was maintained for about 8 h. Thus, a thermoreversible gel formulation that can deliver MOMIPP in animal studies was successfully developed.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Oppong F,Li Z,Fakhrabadi EA,Raorane T,Giri PM,Liberatore MW,Sarver JG,Trabbic CJ,Hosier CE,Erhardt PW,Maltese WA,Nesamony Jdoi
10.1016/j.xphs.2020.05.014subject
Has Abstractpub_date
2020-09-01 00:00:00pages
2719-2728issue
9eissn
0022-3549issn
1520-6017pii
S0022-3549(20)30263-Xjournal_volume
109pub_type
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