Long-Acting Risperidone Dual Control System: Preparation, Characterization and Evaluation In Vitro and In Vivo

Yan, Xieguo; Wang, Shiqiang; Sun, Kaoxiang

doi:10.3390/pharmaceutics13081210

Cited by 5 publications

(6 citation statements)

References 39 publications

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“…However, MP released only 25% of the total Ris encapsulated while MP-R released only 20% of the total Ris encapsulated, within the study period of 10 days. This indicates that the microparticles require a longer time to achieve complete release of Ris, concurring with previous studies that showed prolonged three months release of Ris from PLA microparticles implanted in rats [18].…”

Section: Resultssupporting

confidence: 92%

Ultralong floating hydrogel raft for prolonged gastric retention

2022

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The optimal therapeutic efficiency of any treatment depends on patient adherence to the medication regimen. Medication adherence is the cornerstone of treatment outcomes that may consequently impact economic and healthcare costs. With the oral route being the preferred route of drug administration, slow or extended-release oral formulations can therefore be utilized. Here, a biocompatible oral delivery system that can be retained in the stomach for a week, while providing continuous release of the encased drug, is proposed. The fabrication of the delivery system was achieved using a simple mould casting technique. The hydrogel-based raft was able to float under simulated gastric conditions for seven days with pH switches to mimic the fasted and fed states of the stomach. The functionality of such a delivery system has been exemplified using two different model drugs -Risperidone and Metoprolol tartrate of varied solubilities and has been shown to effectively sustain the release of drugs under the tested conditions. IMPACT STATEMENTAn oral delivery system is proposed to tackle the soaring problem of medication non-adherence predominantly for conditions that require long-term medication. The proposed delivery system is designed to float in the stomach, thereby prolonging gastric retention and sustaining drug release for over a week. Subsequently, once drug release is completed it can be dissolved away using an extrinsic trigger. Any chronic disease condition that requires multiple dosing per day or to be taken over a prolonged period would benefit from such a sustained-releasing drug delivery system. This reduces dosing frequency and consequently improves patient medication compliance. The proposed design allows for easy adaptation to different drugs making it customisable to the patient's needs. The application of the delivery system may also be extended to the delivery and retention of miniature devices, like glucose sensors that are to be retained for an extended period in the body, for the purpose of health monitoring or probing. In addition, this technology could have an impact beyond biomedical/pharmaceutical applications, where the need for extended-release is a requirement. For instance, as a floating device for environmental purposes, i.e., slow release of pesticides into water bodies against mosquito breeding, may be a possibility.

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Section: Resultssupporting

confidence: 92%

Ultralong floating hydrogel raft for prolonged gastric retention

2022

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“…The spectra for risperidone showed the same characteristic peaks as previously mentioned [ 16 ]. FTIR spectroscopy revealed that no extra functional group and bond were observed in the NP forms, and it was evident that RIS was intact and there were no pronounced chemical interactions.…”

Section: Discussionsupporting

confidence: 73%

“…The FTIR spectra of risperidone showed characteristic peaks at 1643 cm −1 due to the stretching of functional groups C=O of aromatic ketone and peak at 1533 cm −1 due to C=C stretching of the arene ring. The peaks at 1396 cm −1 , 1349 cm −1 , 1271 cm −1 , 1192 cm −1 and 1130 cm −1 were due to the functional groups of C-N, C-H, C-F and C-O, respectively [ 16 ]. In polymer spectra, stretchings at 3564 cm −1 , 1750 cm −1 , 1648 cm −1 , 1612 cm −1 , 1534 cm −1 , 1350 cm −1 and 1192 cm −1 indicated the presence of the functional groups O-H, C=O, C=C, C-N, C-F and C-O, respectively.…”

Section: Resultsmentioning

confidence: 99%

Development and Evaluation of PLGA Nanoparticle-Loaded Organogel for the Transdermal Delivery of Risperidone

Dilawar

Ur-Rehman

Shah

et al. 2022

Gels

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A transdermal delivery approach may circumvent the limitations associated with the oral use of risperidone (RIS), an atypical antipsychotic drug. The current study focuses on the utilization of poloxamer (pluronic) lecithin organogel (PLO), a suitable transdermal vehicle, and a biodegradable nanoparticulate system of PLGA with the potential to deliver RIS in an efficient way. PLGA nanoparticles were fabricated using different ratios of the polymer and surfactant. The optimization was performed principally on the basis of particle size and entrapment efficiency (EE). The developed PLGA nanoparticles were spherical, sized around 109 nm with negative charge (−9.3 mv) and enhanced drug entrapment efficiency (58%). The in vitro drug release study of lyophilized nanoparticles showed a sustained pattern. Statistical analysis confirmed that there was a significant difference (p < 0.05) between the nanoparticle-loaded PLO gel and conventional drug formulations in terms of drug release and ex vivo permeation across rat skin (three-fold). The results confirm enhanced drug release and permeation through the skin at 72 h. Hence, the investigated formulation could be a better alternative to the conventional route for improving patient compliance.

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“…Yan et al [ 139 ] evaluated the role of different pore formers, polymer ratios, porogen levels, and oil–water ratios on risperidone release from implantation systems. The authors used cumulative release, drug loading, and entrapment efficiency as assessment indicators.…”

Section: Pharmaceutical Analysis Of Lai Antipsychoticsmentioning

confidence: 99%

Long-Acting Injectable Antipsychotics—A Review on Formulation and In Vitro Dissolution

Markowicz-Piasecka,

Kubisiak,

Asendrych-Wicik

et al. 2023

Pharmaceutics

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Long-acting injectable (LAI) neuroleptics constitute an effective therapeutical alternative for individuals suffering from persistent mental illness. These injectable pharmaceuticals help patients manage their condition better and improve long-term outcomes by preventing relapses and improving compliance. This review aims to analyse the current formulation aspects of LAI neuroleptics, with particular emphasis on analysis of drug release profiles as a critical test to guarantee drug quality and relevant therapeutical activity. While there is no officially approved procedure for depot parenteral drug formulations, various dissolution tests which were developed by LAI manufacturers are described. In vitro dissolution tests also possess a critical function in the estimation of the in vivo performance of a drug formulation. For that reason, thorough inspection of the in vitro–in vivo correlation (IVIVC) is also discussed.

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Long-Acting Risperidone Dual Control System: Preparation, Characterization and Evaluation In Vitro and In Vivo

Cited by 5 publications

References 39 publications

Ultralong floating hydrogel raft for prolonged gastric retention

Ultralong floating hydrogel raft for prolonged gastric retention

Development and Evaluation of PLGA Nanoparticle-Loaded Organogel for the Transdermal Delivery of Risperidone

Long-Acting Injectable Antipsychotics—A Review on Formulation and In Vitro Dissolution

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