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Preparation, Characterization, and In Vivo Evaluation of Olanzapine Poly(D,L-lactide-co-glycolide) Microspheres.

D'Souza S, Faraj JA, Giovagnoli S, DeLuca PP - J Pharm (Cairo) (2013)

Bottom Line: A simulation of multiple dosing at 7- and 10-day intervals for Formulations A and B revealed that steady state was achieved within 7-21 days and 10-30 days, respectively.Similarly, simulations at 15-day intervals for Formulations C and D indicated that steady state levels were reached during days 15-45.Overall, steady state levels for 7-, 10-, or 15-day dosing ranged between 45 and 65 ng/mL for all the formulations, implying that Olanzapine PLGA microspheres can be tailored to treat patients with varying clinical needs.

View Article: PubMed Central - PubMed

Affiliation: Sunovion Pharmaceuticals Inc., Marlborough, MA 01752, USA.

ABSTRACT
The aim of this study was to prepare injectable depot formulations of Olanzapine using four poly(D,L-lactide-co-glycolide) (PLGA) polymers of varying molecular weight and copolymer composition, and evaluate in vivo performance in rats. In vivo release profiles from the formulations were governed chiefly by polymer molecular weight and to a lesser extent, copolymer composition. Formulations A and B, manufactured using low molecular weight PLGA and administered at 10 mg/kg dose, released drug within 15 days. Formulation C, prepared from intermediate molecular weight PLGA and administered at 20 mg/kg dose, released drug in 30 days, while Formulation D, manufactured using a high molecular weight polymer and administered at 20 mg/kg dose, released drug in 45 days. A simulation of multiple dosing at 7- and 10-day intervals for Formulations A and B revealed that steady state was achieved within 7-21 days and 10-30 days, respectively. Similarly, simulations at 15-day intervals for Formulations C and D indicated that steady state levels were reached during days 15-45. Overall, steady state levels for 7-, 10-, or 15-day dosing ranged between 45 and 65 ng/mL for all the formulations, implying that Olanzapine PLGA microspheres can be tailored to treat patients with varying clinical needs.

No MeSH data available.


Scanning electron micrographs of Olanzapine PLGA microspheres.
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Related In: Results  -  Collection


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fig1: Scanning electron micrographs of Olanzapine PLGA microspheres.

Mentions: The SEM images of Formulations A, B, C, and D are provided in Figure 1. The scanning electron micrographs revealed microspheres having a spherical shape with a smooth nonporous surface and homogeneous particle size distribution. Particle size analysis revealed that Formulations A, B, C, and D had a mean volume diameter of 17.0, 16.8, 22.3, and 20.6 μm, respectively (Table 1). The mean volume diameter was similar for Formulations A and B, both prepared from lower molecular weight PLGA, while the same was true for Formulations C and D, manufactured using higher molecular weight PLGA.


Preparation, Characterization, and In Vivo Evaluation of Olanzapine Poly(D,L-lactide-co-glycolide) Microspheres.

D'Souza S, Faraj JA, Giovagnoli S, DeLuca PP - J Pharm (Cairo) (2013)

Scanning electron micrographs of Olanzapine PLGA microspheres.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590816&req=5

fig1: Scanning electron micrographs of Olanzapine PLGA microspheres.
Mentions: The SEM images of Formulations A, B, C, and D are provided in Figure 1. The scanning electron micrographs revealed microspheres having a spherical shape with a smooth nonporous surface and homogeneous particle size distribution. Particle size analysis revealed that Formulations A, B, C, and D had a mean volume diameter of 17.0, 16.8, 22.3, and 20.6 μm, respectively (Table 1). The mean volume diameter was similar for Formulations A and B, both prepared from lower molecular weight PLGA, while the same was true for Formulations C and D, manufactured using higher molecular weight PLGA.

Bottom Line: A simulation of multiple dosing at 7- and 10-day intervals for Formulations A and B revealed that steady state was achieved within 7-21 days and 10-30 days, respectively.Similarly, simulations at 15-day intervals for Formulations C and D indicated that steady state levels were reached during days 15-45.Overall, steady state levels for 7-, 10-, or 15-day dosing ranged between 45 and 65 ng/mL for all the formulations, implying that Olanzapine PLGA microspheres can be tailored to treat patients with varying clinical needs.

View Article: PubMed Central - PubMed

Affiliation: Sunovion Pharmaceuticals Inc., Marlborough, MA 01752, USA.

ABSTRACT
The aim of this study was to prepare injectable depot formulations of Olanzapine using four poly(D,L-lactide-co-glycolide) (PLGA) polymers of varying molecular weight and copolymer composition, and evaluate in vivo performance in rats. In vivo release profiles from the formulations were governed chiefly by polymer molecular weight and to a lesser extent, copolymer composition. Formulations A and B, manufactured using low molecular weight PLGA and administered at 10 mg/kg dose, released drug within 15 days. Formulation C, prepared from intermediate molecular weight PLGA and administered at 20 mg/kg dose, released drug in 30 days, while Formulation D, manufactured using a high molecular weight polymer and administered at 20 mg/kg dose, released drug in 45 days. A simulation of multiple dosing at 7- and 10-day intervals for Formulations A and B revealed that steady state was achieved within 7-21 days and 10-30 days, respectively. Similarly, simulations at 15-day intervals for Formulations C and D indicated that steady state levels were reached during days 15-45. Overall, steady state levels for 7-, 10-, or 15-day dosing ranged between 45 and 65 ng/mL for all the formulations, implying that Olanzapine PLGA microspheres can be tailored to treat patients with varying clinical needs.

No MeSH data available.