Solubility behaviour of haloperidol in individual solvents determination of partial solubility parameters

Subrahmanyam, C.V.S.; Suresh, Sarasija

doi:10.1016/s0939-6411(98)00079-4

Cited by 15 publications

(3 citation statements)

References 8 publications

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“…Furthermore, EM does not account (1 0-1) for the same relevance that the other two computational methods give to this face. As shown in Figure 5 (right), unlike BFDH, the most relevant consequence of these results is that the habit resulting from GM and, even more, the one resulting from EM expose to polar aprotic solvents-that is, the ones in which haloperidol is more soluble 55 -also faces with a majority of apolar groups. Remembering that the crystal packing analysis evidenced the lack of solvent accessible voids in the structure, the attachments of those solvent molecules must take place directly from the outer part of these faces; their attachment is slow and therefore, the slow faces growth in that direction will result in larger faces surface.…”

Section: In Silico Studymentioning

confidence: 94%

How molecular interactions affect crystal morphology: The case of haloperidol

Destri

Marrazzo

Rescifina

et al. 2011

Journal of Pharmaceutical Sciences

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Section: In Silico Studymentioning

confidence: 94%

How molecular interactions affect crystal morphology: The case of haloperidol

Destri

Marrazzo

Rescifina

et al. 2011

Journal of Pharmaceutical Sciences

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“…The parameter between haloperidol and water was obtained [7] by fitting the experimental solubility data to obtain regression equations, which gave a reasonable prediction of the solubility of haloperidol in the solvent. The interaction parameter values are given in Table I.…”

Section: Mesoscale Simulationsmentioning

confidence: 99%

Mesoscale Simulation and cryo-TEM of Nanoscale Drug Delivery Systems

Lam

Goldbeck

Boothroyd

2004

Molecular Simulation

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This work sets out to study the effect of hydrophobic molecules on the morphology of aqueous solutions of amphiphilic block copolymer, which has potential drug delivery applications. The effect is studied both experimentally and by using simulations. Using cryogenic TEM observations, micelles can clearly be visualised and their core size measured. While pure polymer solutions form into spherical micelles with a narrow size distribution, addition of small amounts of hydrophobic drug molecules leads to distortions in shape, a wider size distribution, and larger average core diameter. Simulations are based on a mesoscale dynamic density functional method with Gaussian chain Hamiltonian and mean-field interactions, as implemented in the MesoDyn code. With parameters for the amphiphilic system established in earlier work, and mean-field interactions for the drug molecule derived from structure -property relationships, we obtain good agreement with the TEM observations for the effect of the hydrophobic molecules on the morphology. The simulations clearly show how increasing drug concentration leads to an increase in micelle size, a wider distribution and more elongated rather than spherical micelles.

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“…In this work we examine Eudragit/Brij98 nanocontainers as drug delivery carriers for the encapsulation of haloperidol. Haloperidol is an antipsychotic drug with very poor solubility in water of 14 µg/mL [ 36 , 37 , 38 ]. Several approaches to overcome haloperidol low solubility were suggested recently [ 36 , 39 ].…”

Section: Introductionmentioning

confidence: 99%

Hybrid Nanoparticles for Haloperidol Encapsulation: Quid Est Optimum?

et al. 2021

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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.

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Solubility behaviour of haloperidol in individual solvents determination of partial solubility parameters

Cited by 15 publications

References 8 publications

How molecular interactions affect crystal morphology: The case of haloperidol

How molecular interactions affect crystal morphology: The case of haloperidol

Mesoscale Simulation and cryo-TEM of Nanoscale Drug Delivery Systems

Hybrid Nanoparticles for Haloperidol Encapsulation: Quid Est Optimum?

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