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Polymers 2017, 9(11), 617; https://doi.org/10.3390/polym9110617

Thiolated Chitosan Masked Polymeric Microspheres with Incorporated Mesocellular Silica Foam (MCF) for Intranasal Delivery of Paliperidone

1
Laboratory of Polymer Chemistry and Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece
2
Laboratory of General and Inorganic Chemical Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece
*
Author to whom correspondence should be addressed.
Received: 30 October 2017 / Revised: 8 November 2017 / Accepted: 13 November 2017 / Published: 15 November 2017
(This article belongs to the Special Issue Polymers from Renewable Resources)
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Abstract

In this study, mesocellular silica foam (MCF) was used to encapsulate paliperidone, an antipsychotic drug used in patients suffering from bipolar disorder. MCF with the drug adsorbed was further encapsulated into poly(lactic acid) (PLA) and poly(lactide-co-glycolide) (PLGA) 75/25 w/w microspheres and these have been coated with thiolated chitosan. As found by TEM analysis, thiolated chitosan formed a thin layer on the polymeric microspheres’ surface and was used in order to enhance their mucoadhesiveness. These microspheres aimed at the intranasal delivery of paliperidone. The DSC and XRD studies showed that paliperidone was encapsulated in amorphous form inside the MCF silica and for this reason its dissolution profile was enhanced compared to the neat drug. In coated microspheres, thiolated chitosan reduced the initial burst effect of the paliperidone dissolution profile and in all cases sustained release formulations have been prepared. The release mechanism was also theoretically studied and three kinetic models were proposed and successfully fitted for a dissolution profile of prepared formulations to be found. View Full-Text
Keywords: PLA; PLGA; mesoporous cellular foam; paliperidone; thiolated chitosan; microspheres; drug encapsulation PLA; PLGA; mesoporous cellular foam; paliperidone; thiolated chitosan; microspheres; drug encapsulation
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Nanaki, S.; Tseklima, M.; Christodoulou, E.; Triantafyllidis, K.; Kostoglou, M.; Bikiaris, D.N. Thiolated Chitosan Masked Polymeric Microspheres with Incorporated Mesocellular Silica Foam (MCF) for Intranasal Delivery of Paliperidone. Polymers 2017, 9, 617.

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