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Development of a novel 3-month drug releasing risperidone microspheres.

Yerragunta B, Jogala S, Chinnala KM, Aukunuru J - J Pharm Bioallied Sci (2015 Jan-Mar)

Bottom Line: Microspheres prepared using a blend of PCL-45000 and PCL-80000 at a ratio of 1:1 resulted in the release of the drug in a time frame of 90 days, demonstrated zero-order drug release without lag time and burst release.The optimized formulation also released the drug in vivo for a period of 90 days.From our study, it was concluded that these optimized microspheres showed great potential for a better depot preparation than the marketed Risperdal Consta™ and, therefore, could further improve patient compliance.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Mother Teresa College of Pharmacy, Osmania University, Hyderabad, India.

ABSTRACT

Objective: The purpose of this study was to develop an ideal microsphere formulation of risperidone that would prolong the drug release for 3 months in vivo and avoid the need for co-administration of oral tablets.

Materials and methods: Polycaprolactones (PCL) were used as polymers to prepare microspheres. The research included screening and optimizing of suitable commercial polymers of variable molecular weights: PCL-14000, PCL-45000, PCL-80000 or the blends of these polymers to prepare microspheres with zero-order drug-releasing properties without the lag phase. In the present study, the sustained release risperidone microspheres were prepared by o/w emulsion solvent evaporation technique and the yield was determined. Microspheres were evaluated for their drug content and in vitro drug release. Microspheres prepared using a blend of PCL-45000 and PCL-80000 at a ratio of 1:1 resulted in the release of the drug in a time frame of 90 days, demonstrated zero-order drug release without lag time and burst release. This formulation was considered optimized formulation. Optimized formulation was characterized for solid state of the drug using differential scanning calorimetry, surface morphology using scanning electron microscopy and in vivo drug release in rats.

Results: The surface of the optimized formulation was smooth, and the drug changed its physical form in the presence of blends of polymers and upon fabrication of microspheres. The optimized formulation also released the drug in vivo for a period of 90 days.

Conclusions: From our study, it was concluded that these optimized microspheres showed great potential for a better depot preparation than the marketed Risperdal Consta™ and, therefore, could further improve patient compliance.

No MeSH data available.


Related in: MedlinePlus

Plasma profile of the drug after administration of F5 microspheres and risperdal consta in the rats
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Figure 5: Plasma profile of the drug after administration of F5 microspheres and risperdal consta in the rats

Mentions: In the in vivo studies, plasma concentration at various time points was assessed upon administration of F5 formulation. In vivo, onset was rapid, and plasma concentration was in the range of 15-110 ng/ml for a substantial portion of release interval. Optimized microspheres released the drug for 3 months in vivo [Figure 5]. Risperdal Consta also demonstrated similar results. However, in this case, corroborating in vitro release, sustained in vivo release was also noted for 50 days and the formulation demonstrated significant lag time. Higher plasma levels, when compared to optimized formulation, were achieved with Risperdal Consta. In the pharmacodynamic assessment, the animals were observed for first 1-week to evaluate the signs of high initial drug release. There were no signs of distress during this time. There was no locomotor impairment, no difficulties in grooming, no loss of weight, ate and drank appropriately upon administration of microspheres. This suggested that there was no high initial drug release. In the assessment of locomotor activity, compared to control the group, there was a significant decrease in the locomotor activity of the rats administered microspheres during all the 3 months suggesting the presence of the drug in the plasma during this period, time, term [Figure 6].


Development of a novel 3-month drug releasing risperidone microspheres.

Yerragunta B, Jogala S, Chinnala KM, Aukunuru J - J Pharm Bioallied Sci (2015 Jan-Mar)

Plasma profile of the drug after administration of F5 microspheres and risperdal consta in the rats
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4333626&req=5

Figure 5: Plasma profile of the drug after administration of F5 microspheres and risperdal consta in the rats
Mentions: In the in vivo studies, plasma concentration at various time points was assessed upon administration of F5 formulation. In vivo, onset was rapid, and plasma concentration was in the range of 15-110 ng/ml for a substantial portion of release interval. Optimized microspheres released the drug for 3 months in vivo [Figure 5]. Risperdal Consta also demonstrated similar results. However, in this case, corroborating in vitro release, sustained in vivo release was also noted for 50 days and the formulation demonstrated significant lag time. Higher plasma levels, when compared to optimized formulation, were achieved with Risperdal Consta. In the pharmacodynamic assessment, the animals were observed for first 1-week to evaluate the signs of high initial drug release. There were no signs of distress during this time. There was no locomotor impairment, no difficulties in grooming, no loss of weight, ate and drank appropriately upon administration of microspheres. This suggested that there was no high initial drug release. In the assessment of locomotor activity, compared to control the group, there was a significant decrease in the locomotor activity of the rats administered microspheres during all the 3 months suggesting the presence of the drug in the plasma during this period, time, term [Figure 6].

Bottom Line: Microspheres prepared using a blend of PCL-45000 and PCL-80000 at a ratio of 1:1 resulted in the release of the drug in a time frame of 90 days, demonstrated zero-order drug release without lag time and burst release.The optimized formulation also released the drug in vivo for a period of 90 days.From our study, it was concluded that these optimized microspheres showed great potential for a better depot preparation than the marketed Risperdal Consta™ and, therefore, could further improve patient compliance.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Mother Teresa College of Pharmacy, Osmania University, Hyderabad, India.

ABSTRACT

Objective: The purpose of this study was to develop an ideal microsphere formulation of risperidone that would prolong the drug release for 3 months in vivo and avoid the need for co-administration of oral tablets.

Materials and methods: Polycaprolactones (PCL) were used as polymers to prepare microspheres. The research included screening and optimizing of suitable commercial polymers of variable molecular weights: PCL-14000, PCL-45000, PCL-80000 or the blends of these polymers to prepare microspheres with zero-order drug-releasing properties without the lag phase. In the present study, the sustained release risperidone microspheres were prepared by o/w emulsion solvent evaporation technique and the yield was determined. Microspheres were evaluated for their drug content and in vitro drug release. Microspheres prepared using a blend of PCL-45000 and PCL-80000 at a ratio of 1:1 resulted in the release of the drug in a time frame of 90 days, demonstrated zero-order drug release without lag time and burst release. This formulation was considered optimized formulation. Optimized formulation was characterized for solid state of the drug using differential scanning calorimetry, surface morphology using scanning electron microscopy and in vivo drug release in rats.

Results: The surface of the optimized formulation was smooth, and the drug changed its physical form in the presence of blends of polymers and upon fabrication of microspheres. The optimized formulation also released the drug in vivo for a period of 90 days.

Conclusions: From our study, it was concluded that these optimized microspheres showed great potential for a better depot preparation than the marketed Risperdal Consta™ and, therefore, could further improve patient compliance.

No MeSH data available.


Related in: MedlinePlus