Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Comparative Study
. 2015 Oct;16(5):1129-39.
doi: 10.1208/s12249-015-0305-1. Epub 2015 Feb 21.

Stability Evaluation of Ivermectin-Loaded Biodegradable Microspheres

Rossella Dorati  1 , Ida Genta  1 , Barbara Colzani  1 , Tiziana Modena  1 , Giovanna Bruni  2 , Giuseppe Tripodo  1 , Bice Conti  3
Affiliations
Comparative Study

Stability Evaluation of Ivermectin-Loaded Biodegradable Microspheres

Rossella Dorati et al. AAPS PharmSciTech. 2015 Oct.

Abstract

A stability study was performed on ivermectin (IVM)-loaded biodegradable microparticles intended for injection in dogs. The rational was to evaluate the performances upon irradiation of a drug, such as IVM, with a few criticalities with respect to its stability, and toxicity. The goal was to provide valuable information for pharmaceutical scientists and manufacturers working in the veterinary area. The microspheres based on poly(D,L-lactide) and poly-(ε-caprolactone) and loaded with IVM and with the addition of alpha-tocopherol (TCP) as antioxidant were prepared by the emulsion solvent evaporation method and sterilized by gamma irradiation. Microsphere characterization in term of size, shape, polymer, and IVM stability upon irradiation was performed. The results show that the type of polymer significantly affects microsphere characteristics and performances. Moreover, suitably stable formulations can be achieved only by TCP addition.

Keywords: alpha-tocopherol; gamma irradiation; ivermectin; microspheres; poly(D,L-lactide); poly-(ε-caprolactone).

PubMed Disclaimer

Figures

Fig. 1
Fig. 1
SEM images of a IVM1TCP at ×80 and c IVM1TCP at 1.04 kX magnifications before irradiation; b IVM4TCP at ×82 and IVM4TCP at ×728 magnifications before irradiation; e IVM1TCP at 1.04 kX magnification after irradiation; f IVM4TCP at ×524 magnification after irradiation
Fig. 2
Fig. 2
Schematic representation of the suggested polymer degradation mechanism: a random chain scission and b unzipping
Fig. 3
Fig. 3
HPLC chromatograms of IVM from standard solution (IVM), and from batches IVM1 and IVM1TCP: red line before irradiation and in blue line after irradiation
Fig. 4
Fig. 4
Magnification of HPLC chromatograms of irradiated IVM from: a batch IVM1 and b batch IVM4, before irradiation (red line) and after irradiation (blue lines)
See this image and copyright information in PMC

References

    1. Dorati R, Genta I, Colzani B, Tripodo G, Conti B. Preliminary investigation on the design of biodegradable microparticles for Ivermectin delivery: set up of formulation parameters. Drug Dev Ind Pharm. 2014; 1–11 (early online) doi: 10.3109/03639045.2014.935395. - PubMed
    1. Camargo JA, Sapin A, Nouvel C, Daloz D, Leonard M, Bonneaux F, et al. Injectable PLA-based in situ forming implants for controlled release of Ivermectin a BCS Class II drug: solvent selection based on physico-chemical characterization. Drug Dev Ind Pharm. 2013;39(1):146–55. doi: 10.3109/03639045.2012.660952. - DOI - PubMed
    1. The use of ionizing radiation in the manufacture of medicinal products European Guidelines 3AQ4a.
    1. Conti B, Dorati R, Colonna C, Genta I. Effects of ionizing radiation sterilization on microparticulate drug delivery systems based on poly-α-hydroxyacids: an overview. J Drug Deliv Sci Technol. 2009;19(2):99–112. doi: 10.1016/S1773-2247(09)50017-2. - DOI
    1. Loo JSC, Ooi CP, Boey FYC. Degradation of poly(lactide-co-glycolide) (PLGA) and poly(L-lactide) (PLLA) by electron beam radiation. Biomaterials. 2005;26:1359–67. doi: 10.1016/j.biomaterials.2004.05.001. - DOI - PubMed

Publication types