PMID- 27793717 OWN - NLM STAT- MEDLINE DCOM- 20170406 LR - 20170904 IS - 1879-0720 (Electronic) IS - 0928-0987 (Linking) VI - 96 DP - 2017 Jan 1 TI - Synergistic role of solid lipid and porous silica in improving the oral delivery of weakly basic poorly water soluble drugs. PG - 508-514 LID - S0928-0987(16)30465-1 [pii] LID - 10.1016/j.ejps.2016.10.026 [doi] AB - Oral absorption of weakly basic drugs (e.g. cinnarizine (CIN)) is limited by their pH dependent precipitation in intestinal conditions. To overcome this challenge, a novel drug delivery system composed of solid lipid and porous silica, namely silica encapsulated solid lipid (SESL) particles, was developed via hot homogenization of melted lipid dispersion, followed by ultra-sonication of the silica stabilized homogenized melted lipid dispersion. Scanning electron microscope (SEM) images of the SESL formulation revealed non-spherical and aggregated hybrid particles, with rough exterior and structured nanoparticles visible on the surface. A 1.5, 2.2 and 7-fold improvement in the dissolution of CIN was observed for the SESL particles, under simulated intestinal non-digesting conditions, in comparison to the drug loaded in solid lipid (CIN-SL) matrix, drug loaded in porous silica (CIN-PS) and pure drug powder. Under simulated intestinal digestive condition, significant improvement in the drug solubilization was reported for the SESL formulation in compared to the individual drug loaded systems i.e. CIN-PS and CIN-SL. Thereby, silica encapsulated solid lipid system provides a promising oral delivery approach for poorly water soluble weakly basic drugs. CI - Copyright (c) 2016 Elsevier B.V. All rights reserved. FAU - Yasmin, Rokhsana AU - Yasmin R AD - School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia 5000, Australia. FAU - Rao, Shasha AU - Rao S AD - School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia 5000, Australia. FAU - Bremmell, Kristen AU - Bremmell K AD - School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia 5000, Australia. FAU - Prestidge, Clive AU - Prestidge C AD - School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia 5000, Australia. Electronic address: Clive.Prestidge@unisa.edu.au. LA - eng PT - Journal Article DEP - 20161026 PL - Netherlands TA - Eur J Pharm Sci JT - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JID - 9317982 RN - 0 (Drug Carriers) RN - 0 (Lipids) RN - 059QF0KO0R (Water) RN - 3DI2E1X18L (Cinnarizine) RN - 7631-86-9 (Silicon Dioxide) SB - IM MH - Administration, Oral MH - Cinnarizine/administration & dosage/*chemistry/pharmacokinetics MH - Drug Carriers/administration & dosage/*chemistry/pharmacokinetics MH - Drug Delivery Systems/*methods MH - Drug Synergism MH - Hydrogen-Ion Concentration MH - Lipids/administration & dosage/*chemistry/pharmacokinetics MH - Porosity MH - Silicon Dioxide/administration & dosage/*chemistry/pharmacokinetics MH - Solubility MH - Water/metabolism OTO - NOTNLM OT - Oral delivery OT - Poorly water soluble drugs OT - Porous silica OT - Solid lipid OT - Solubilization EDAT- 2016/10/30 06:00 MHDA- 2017/04/07 06:00 CRDT- 2016/10/30 06:00 PHST- 2016/08/24 00:00 [received] PHST- 2016/10/20 00:00 [revised] PHST- 2016/10/22 00:00 [accepted] PHST- 2016/10/30 06:00 [pubmed] PHST- 2017/04/07 06:00 [medline] PHST- 2016/10/30 06:00 [entrez] AID - S0928-0987(16)30465-1 [pii] AID - 10.1016/j.ejps.2016.10.026 [doi] PST - ppublish SO - Eur J Pharm Sci. 2017 Jan 1;96:508-514. doi: 10.1016/j.ejps.2016.10.026. Epub 2016 Oct 26.