Facilitating Gastrointestinal Solubilisation and Enhanced Oral Absorption of SN38 Using a Molecularly Complexed Silica-Lipid Hybrid Delivery System

SN38 (7-ethyl-10-hydroxycamptothecin) is a highly potent anti-cancer compound. However, it is poorly soluble in pharmaceutically acceptable excipients, thus the direct formulation and delivery is restricted. The current study focused on lipid-based formulation design to enable oral delivery of SN38 at high doses and at therapeutic levels. The pH dependent ionisation property of SN38 was utilized to form a molecular complex with the cationic surfactant, oleylamine and this increased (> 200-fold) solubility/loading in Labrasol (the optimally determined lipid carrier). A SN38 loaded silica-lipid hybrid (SN38-SLH) particle delivery system was prepared by lyophilisation of mesoporous silica nanoparticle stabilised lipid emulsions.

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