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Hybrid Nanoparticles for Haloperidol Encapsulation: Quid Est Optimum?

Pharmaceutical Sciences Laboratory and Turku Bioscience Center, Åbo Akademi University, 20520 Turku, Finland
Turku Bioscience Center, University of Turku, 20520 Turku, Finland
School of Pharmacy, University of Reading, Whiteknights, Reading RG6 6AD, UK
Institute of Pharmacy, Kazan State Medical University, 16 Fatykh Amirkhan, 420126 Kazan, Russia
Department of Pharmacology, Kazan State Medical University, 49 Butlerov str., 420012 Kazan, Russia
Heinz Maier-Leibnitz Zentrum (MLZ), Technische Universität München, Lichtenbergstraße 1, 85748 Garching, Germany
Authors to whom correspondence should be addressed.
Academic Editor: Ki Hyun Bae
Polymers 2021, 13(23), 4189;
Received: 25 October 2021 / Revised: 23 November 2021 / Accepted: 26 November 2021 / Published: 30 November 2021
(This article belongs to the Section Polymer Networks)
The choice of drug delivery carrier is of paramount importance for the fate of a drug in a human body. In this study, we have prepared the hybrid nanoparticles composed of FDA-approved Eudragit L100-55 copolymer and polymeric surfactant Brij98 to load haloperidol—an antipsychotic hydrophobic drug used to treat schizophrenia and many other disorders. This platform shows good drug-loading efficiency and stability in comparison to the widely applied platforms of mesoporous silica (MSN) and a metal–organic framework (MOF). ZIF8, a biocompatible MOF, failed to encapsulate haloperidol, whereas MSN only showed limited encapsulation ability. Isothermal titration calorimetry showed that haloperidol has low binding with the surface of ZIF8 and MSN in comparison to Eudragit L100-55/Brij98, thus elucidating the striking difference in haloperidol loading. With further optimization, the haloperidol loading efficiency could reach up to 40% in the hybrid Eudragit L100-55/Brij98 nanoparticles with high stability over several months. Differential scanning calorimetry studies indicate that the encapsulated haloperidol stays in an amorphous state inside the Eudragit L100-55/Brij98 nanoparticles. Using a catalepsy and open field animal tests, we proved the prolongation of haloperidol release in vivo, resulting in later onset of action compared to the free drug. View Full-Text
Keywords: Eudragits; haloperidol; antipsychotic drug; nanoparticles; hybrid; SANS; ITC; TEM; mDSC; DLS; MSN Eudragits; haloperidol; antipsychotic drug; nanoparticles; hybrid; SANS; ITC; TEM; mDSC; DLS; MSN
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MDPI and ACS Style

Filippov, S.K.; Khusnutdinov, R.R.; Inham, W.; Liu, C.; Nikitin, D.O.; Semina, I.I.; Garvey, C.J.; Nasibullin, S.F.; Khutoryanskiy, V.V.; Zhang, H.; Moustafine, R.I. Hybrid Nanoparticles for Haloperidol Encapsulation: Quid Est Optimum? Polymers 2021, 13, 4189.

AMA Style

Filippov SK, Khusnutdinov RR, Inham W, Liu C, Nikitin DO, Semina II, Garvey CJ, Nasibullin SF, Khutoryanskiy VV, Zhang H, Moustafine RI. Hybrid Nanoparticles for Haloperidol Encapsulation: Quid Est Optimum? Polymers. 2021; 13(23):4189.

Chicago/Turabian Style

Filippov, Sergey K., Ramil R. Khusnutdinov, Wali Inham, Chang Liu, Dmitry O. Nikitin, Irina I. Semina, Christopher J. Garvey, Shamil F. Nasibullin, Vitaliy V. Khutoryanskiy, Hongbo Zhang, and Rouslan I. Moustafine. 2021. "Hybrid Nanoparticles for Haloperidol Encapsulation: Quid Est Optimum?" Polymers 13, no. 23: 4189.

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