The aim was to design sterile biodegradable microparticulate drug delivery systems based on poly(DL-lactide) (PLA) and poly(-caprolactone) (PCL) and containing ivermectin (IVM), an antiparasitic drug, for subcutaneous administration in dogs. The drug delivery system should: (i) ensure a full 12-month protection upon single dose administration; (ii) be safe with particular attention regarding IVM dosage and its release, in order to prevent over dosage side effects. This preliminary work involves: polymer selection, evaluation of the effects of γ-irradiation on the polymers and IVM, investigation and set up of suitable microparticle preparation process and parameters, IVM-loaded microparticles in vitro release evaluation. Results of gel permeation chromatography analysis on the irradiated polymers and IVM mixtures showed that combination of IVM with the antioxidant α-tocopherol (TCP) reduces the damage extent induced by irradiation treatment, independently on the polymer type. Solvent evaporation process was successfully used for the preparation of PLA microparticles and appropriately modified; it was recognized as suitable for the preparation of PCL microparticles. Good process yields were achieved ranging from 76.08% to 94.72%; encapsulation efficiency was between 85.76% and 91.25%, independently from the polymer used. The type of polymer and the consequent preparation process parameters affected microparticle size that was bigger for PCL microparticles (480-800 μm) and solvent residual that was >500 ppm for PLA microparticles. In vitro release test showed significantly faster IVM release rates from PCL microparticles, with respect to PLA microparticles, suggesting that a combination of the polymers could be used to obtain the suitable drug release rate.

Dorati, R., Genta, I., Colzani, B., Tripodo, G., Conti, B. (2015). Preliminary investigation on the design of biodegradable microparticles for ivermectin delivery: Set up of formulation parameters. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 41(7), 1182-1192 [10.3109/03639045.2014.935395].

Preliminary investigation on the design of biodegradable microparticles for ivermectin delivery: Set up of formulation parameters

COLZANI, BARBARA;
2015

Abstract

The aim was to design sterile biodegradable microparticulate drug delivery systems based on poly(DL-lactide) (PLA) and poly(-caprolactone) (PCL) and containing ivermectin (IVM), an antiparasitic drug, for subcutaneous administration in dogs. The drug delivery system should: (i) ensure a full 12-month protection upon single dose administration; (ii) be safe with particular attention regarding IVM dosage and its release, in order to prevent over dosage side effects. This preliminary work involves: polymer selection, evaluation of the effects of γ-irradiation on the polymers and IVM, investigation and set up of suitable microparticle preparation process and parameters, IVM-loaded microparticles in vitro release evaluation. Results of gel permeation chromatography analysis on the irradiated polymers and IVM mixtures showed that combination of IVM with the antioxidant α-tocopherol (TCP) reduces the damage extent induced by irradiation treatment, independently on the polymer type. Solvent evaporation process was successfully used for the preparation of PLA microparticles and appropriately modified; it was recognized as suitable for the preparation of PCL microparticles. Good process yields were achieved ranging from 76.08% to 94.72%; encapsulation efficiency was between 85.76% and 91.25%, independently from the polymer used. The type of polymer and the consequent preparation process parameters affected microparticle size that was bigger for PCL microparticles (480-800 μm) and solvent residual that was >500 ppm for PLA microparticles. In vitro release test showed significantly faster IVM release rates from PCL microparticles, with respect to PLA microparticles, suggesting that a combination of the polymers could be used to obtain the suitable drug release rate.
Articolo in rivista - Articolo scientifico
Biodegradable polymers; ionizing irradiation; ivermectin; microspheres; poly(DL-lactide); poly(ε-caprolactone); Animals; Antiparasitic Agents; Chemistry, Pharmaceutical; Delayed-Action Preparations; Dog Diseases; Dogs; Drug Carriers; Drug Delivery Systems; Ivermectin; Microspheres; Particle Size; Polyesters; Solvents; Medicine (all); Pharmacology; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry
English
2015
41
7
1182
1192
none
Dorati, R., Genta, I., Colzani, B., Tripodo, G., Conti, B. (2015). Preliminary investigation on the design of biodegradable microparticles for ivermectin delivery: Set up of formulation parameters. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 41(7), 1182-1192 [10.3109/03639045.2014.935395].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/147727
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