3-month parenteral PLGA microsphere formulations of risperidone: Fabrication, characterization and neuropharmacological assessments

Chaurasia, Sundeep; Mounika, K.; Bakshi, Vasudha; Prasad, Vure

doi:10.1016/j.msec.2017.03.065

Cited by 15 publications

(11 citation statements)

References 35 publications

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“…A 3M bio-adhesive was added to the wound and closed with pressure for 30 s, followed by rubbing with 75% ethanol. The first group of rats (n = 30) was administered doses equivalent to 50 mg RIS [ 18 ], of which 12 rats were used only for pharmacokinetics and 18 were used for degradation studies in polymers. The second group of rats (n = 12) received a dose equivalent to 25 mg RIS.…”

Section: Methodsmentioning

confidence: 99%

“…Furthermore, polyurethane and poly lactic-co-glycolic acid (PLGA) have been used as slow-release materials. Researchers have recently developed long-acting RIS microspheres, which gradually release RIS for up to 3 months and do not have the drawbacks of oral tablets [ 17 , 18 ]. Although these studies did not determine the ideal long-acting preparation of RIS, they provided guidance for further studies.…”

Section: Introductionmentioning

confidence: 99%

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

Yan

Wang²,

Sun

2021

Pharmaceutics

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Schizophrenia, a psychiatric disorder, requires long-term treatment; however, large fluctuations in blood drug concentration increase the risk of adverse reactions. We prepared a long-term risperidone (RIS) implantation system that can stabilize RIS release and established in-vitro and in-vivo evaluation systems. Cumulative release, drug loading, and entrapment efficiency were used as evaluation indicators to evaluate the effects of different pore formers, polymer ratios, porogen concentrations, and oil–water ratios on a RIS implant (RIS-IM). We also built a mathematical model to identify the optimized formulation by stepwise regression. We also assessed the crystalline changes, residual solvents, solubility and stability after sterilization, in-vivo polymer degradation, pharmacokinetics, and tissue inflammation in the case of the optimized formulation. The surface of the optimized RIS microspheres was small and hollow with 134.4 ± 3.5 µm particle size, 1.60 SPAN, 46.7% ± 2.3% implant drug loading, and 93.4% entrapment efficiency. The in-vitro dissolution behavior of RIS-IM had zero-order kinetics and stable blood concentration; no lag time was released for over three months. Furthermore, the RIS-IM was not only non-irritating to tissues but also had good biocompatibility and product stability. Long-acting RIS-IMs with microspheres and film coatings can provide a new avenue for treating schizophrenia.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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

Yan

Wang²,

Sun

2021

Pharmaceutics

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“…Research on such drug delivery systems has been growing increasingly in the last decades due to the several advantages that they possess, including better patient compliance through lower dosing frequency, consistent drug blood levels, reduced adverse effects, avoidance of first-pass metabolism etc. [ 5 ]. Especially in the case of schizophrenia, important new formulation approaches in the area of drug delivery have been introduced since the first conventional depot formulation for the delivery of an antipsychotic API was introduced [ 6 ].…”

Section: Introductionmentioning

confidence: 99%

Risperidone Controlled Release Microspheres Based on Poly(Lactic Acid)-Poly(Propylene Adipate) Novel Polymer Blends Appropriate for Long Acting Injectable Formulations

et al. 2018

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The present study evaluates the preparation of risperidone controlled release microspheres as appropriate long-acting injectable formulations based on a series of novel biodegradable and biocompatible poly(lactic acid)–poly(propylene adipate) (PLA/PPAd) polymer blends. Initially, PPAd was synthesized using a two-stage melt polycondensation method (esterification and polycondensation) and characterized by 1H-NMR, differential scanning calorimetry (DSC), and powder X-ray diffraction (XRD) analyses. DSC and XRD results for PLA/PPAd blends (prepared by the solvent evaporation method) showed that these are immiscible, while enzymatic hydrolysis studies performed at 37 °C showed increased mass loss for PPAd compared to PLA. Risperidone-polyester microparticles prepared by the oil–water emulsification/solvent evaporation method showed smooth spherical surface with particle sizes from 1 to 15 μm. DSC, XRD, and Fourier-transformed infrared (FTIR) analyses showed that the active pharmaceutical ingredient (API) was dispersed in the amorphous phase within the polymer matrices, whereas in vitro drug release studies showed risperidone controlled release rates in all PLA/PPAd blend formulations. Finally, statistical moment analysis showed that polyester hydrolysis had a major impact on API release kinetics, while in PLA/PPAd blends with high PLA content, drug release was mainly controlled by diffusion.

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“…The diffusion of the drug through the dialysis membrane into the outer medium can be affected by stirring the contents of the container, thus minimizing the effect of the unagitated water layer [ 16 ]. Commonly used modes of agitation include a shaker [ 49 , 50 ], magnetic stirrer [ 51 , 52 ], and the United States Pharmacopeia (USP) paddle apparatus under agitation [ 53 ]. Unlike regular dialysis, reverse dialysis is a method where the microparticles are placed outside the dialysis tubing and sampling is performed inside the dialysis tubing containing only the medium [ 54 , 55 ].…”

Section: In Vitro Drug Release Testing Methodsmentioning

confidence: 99%

“…Nonetheless, the selection of MWCO is somewhat subjective because the criteria are not clear. For example, MWCO of 3.5–5 kDa for loperamide [ 57 ], 8–14 kDa for risperidone [ 51 ], cyclic somatostatin [ 58 ] and cefquinome [ 59 ], and 100 kDa for beta-sheet peptide [ 60 ] have been used. The volume contained in the dialysis bag is much smaller than the external medium.…”

Section: In Vitro Drug Release Testing Methodsmentioning

confidence: 99%

Recent Progress in Drug Release Testing Methods of Biopolymeric Particulate System

et al. 2021

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Biopolymeric microparticles have been widely used for long-term release formulations of short half-life chemicals or synthetic peptides. Characterization of the drug release from microparticles is important to ensure product quality and desired pharmacological effect. However, there is no official method for long-term release parenteral dosage forms. Much work has been done to develop methods for in vitro drug release testing, generally grouped into three major categories: sample and separate, dialysis membrane, and continuous flow (flow-through cell) methods. In vitro drug release testing also plays an important role in providing insight into the in vivo performance of a product. In vitro release test with in vivo relevance can reduce the cost of conducting in vivo studies and accelerate drug product development. Therefore, investigation of the in vitro–in vivo correlation (IVIVC) is increasingly becoming an essential part of particulate formulation development. This review summarizes the principles of the in vitro release testing methods of biopolymeric particulate system with the recent research articles and discusses their characteristics including IVIVC, accelerated release testing methods, and stability of encapsulated drugs.

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3-month parenteral PLGA microsphere formulations of risperidone: Fabrication, characterization and neuropharmacological assessments

Cited by 15 publications

References 35 publications

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

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

Risperidone Controlled Release Microspheres Based on Poly(Lactic Acid)-Poly(Propylene Adipate) Novel Polymer Blends Appropriate for Long Acting Injectable Formulations

Recent Progress in Drug Release Testing Methods of Biopolymeric Particulate System

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