Modeling the Kinetics of Release of Octreotide from Long‐Acting Formulations Injected Intramuscularly in Rabbits

Comets, Emmanuelle; Kawai, Ryoji; Nimmerfall, Fritz; Marbach, Peter; Vonderscher, Jacky

doi:10.1002/1520-6017(200009)89:9<1123::aid-jps4>3.0.co;2-k

Cited by 14 publications

(12 citation statements)

References 15 publications

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“…Similar release patterns from rabbits and humans were observed. [26] Methods for the preparation of PLGA and its co-polymerbased nanoparticles Three well-developed methods exist for the preparation of nanoparticles using PLGA and its co-polymer. [5] These include emulsification solvent diffusion/evaporation, [27,28] salting out [29] and nanoprecipitation.…”

Section: Plga In Drug Delivery Systemsmentioning

confidence: 99%

Nanoparticles based on PLGA and its co-polymer: An overview

Muthu¹

2009

Asian J Pharm

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P oly (D, L-lactide-co-glycolide) (PLGA) is approved by the Food and Drug Administration for drug delivery use. The polymeric nanoparticles based on PLGA and its co-polymer are designed for controlled and targeted drug delivery. Also, PLGA and its co-polymer are important in designing nanoparticles with desired characteristics such as biocompatibility, biodegradation, particle size, surface properties, drug release and targetability. This review focuses on the polymer literature, methods for preparation of nanoparticles and recent studies on the nanoparticles based on PLGA and its co-polymer for the conventional and targeted delivery of drugs by various routes.

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Section: Plga In Drug Delivery Systemsmentioning

confidence: 99%

Nanoparticles based on PLGA and its co-polymer: An overview

Muthu¹

2009

Asian J Pharm

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“…So it was reasonable to observe that the release of PLGAbased system in vivo was faster than that in vitro (Machida et al, 2000;Jiang et al, 2003) because degradation of PLGA in vivo was faster than that in vitro due to the foreign body response (Spenlehauer et al, 1989;Tracy et al, 1999). It is shown in several literatures that drug release from microspheres in animal correlates very well with drug release in human (Periti et al, 2002;Comets et al, 2000). In this study, IFN␣-2b release from the microspheres in rats has shown to be fairly constant, especially in the last 12 days, so it is reasonable to anticipate that the microspheres will provide a fairly constant rate of IFN␣-2b release in human and provide stable effect for above 10 days.…”

Section: In Vivo Release In Ratsmentioning

confidence: 99%

Development of interferon alpha-2b microspheres with constant release

Li¹,

Liu³

et al. 2011

International Journal of Pharmaceutics

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“…More significantly, the gamma irradiation effects did not influence the in vivo release kinetics and performance of the formulation. It has been reported in the literature that there is good correlation of the in vivo drug release from microsphere systems in rabbits and humans (34,35).…”

Section: Pharmacokinetic Studymentioning

confidence: 99%

Formulation and Performance Characterization of Radio-Sterilized “Progestin-Only” Microparticles Intended for Contraception

Puthli

Vavia

2009

AAPS PharmSciTech

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Abstract. The aim of this study was to formulate and characterize a microparticulate system of progestinonly contraceptive. Another objective was to evaluate the effect of gamma radio-sterilization on in vitro and in vivo drug release characteristics. Levonorgestrel (LNG) microspheres were fabricated using poly (lactide-co-glycolide) (PLGA) by a novel solvent evaporation technique. The formulation was optimized for drug/polymer ratio, emulsifier concentration, and process variables like speed of agitation and evaporation method. The drug to polymer ratio of 1:5 gave the optimum encapsulation efficiency. Speed of agitation influenced the spherical shape of the microparticles, lower speeds yielding less spherical particles. The speed did not have a significant influence on the drug payloads. A combination of stabilizers viz. methyl cellulose and poly vinyl alcohol with in-water solvent evaporation technique yielded microparticles without any free drug crystals on the surface. This aspect significantly eliminated the in vitro dissolution "burst effect". The residual solvent content was well within the regulatory limits. The microparticles passed the test for sterility and absence of pyrogens. In vitro dissolution conducted on the product before and after gamma radiation sterilization at 2.5 Mrad indicated no significant difference in the drug release patterns. The drug release followed zero-order kinetics in both static and agitation conditions of dissolution testing. The in vivo studies conducted in rabbits exhibited LNG release up to 1 month duration with drug levels maintained within the effective therapeutic window.

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Modeling the Kinetics of Release of Octreotide from Long‐Acting Formulations Injected Intramuscularly in Rabbits

Cited by 14 publications

References 15 publications

Nanoparticles based on PLGA and its co-polymer: An overview

Nanoparticles based on PLGA and its co-polymer: An overview

Development of interferon alpha-2b microspheres with constant release

Formulation and Performance Characterization of Radio-Sterilized “Progestin-Only” Microparticles Intended for Contraception

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