Abstract：
:Hydroxyethyl bearing gemini surfactants, alkanediyl-α,ω-bis(N-hexadecyl-N-2-hydroxyethyl-N-methylammonium bromide), 16-s-16(OH), were used to augment phosphatidylcholine based liposomes to achieve higher stability and enhanced cellular uptake and penetration. The developed liposomes were loaded with rhodamine B, doxorubicin hydrochloride, pralidoxime chloride to investigate release properties, cytotoxicity in vitro, as well as ability to cross the blood-brain barrier. At molar ratio of 35:1 (lipid:surfactant) the formulation was found to be of low toxicity, stable for two months, and able to deliver rhodamine B beyond the blood-brain barrier in rats. In vivo, pharmacokinetics of free and formulated 2-PAM in plasma and brain were evaluated, liposomal 2-PAM was found to reactivate 27% of brain acetylcholinesterase, which is, to our knowledge, the first example of such high degree of reactivation after intravenous administration of liposomal drug.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Pavlov RV,Gaynanova GA,Kuznetsova DA,Vasileva LA,Zueva IV,Sapunova AS,Buzyurova DN,Babaev VM,Voloshina AD,Lukashenko SS,Rizvanov IK,Petrov KA,Zakharova LY,Sinyashin OGdoi
10.1016/j.ijpharm.2020.119640subject
Has Abstractpub_date
2020-09-25 00:00:00pages
119640eissn
0378-5173issn
1873-3476pii
S0378-5173(20)30624-4journal_volume
587pub_type
杂志文章abstract：PURPOSE:Application of spray-dried chitinosans as excipients for use in drug delivery systems was explored. METHODS:Spray- and tray-dried chitinosans previously N-deacetylated and depolymerized were used. Directly compressed tablets (200mg) containing tetracycline, chitinosan, and magnesium stearate were prepared. The...
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