Next Article in Journal
Scientia Pharmaceutica, Autorenhinweise 2014
Previous Article in Journal
Dissolution Improvement of Atorvastatin Calcium using Modified Locust Bean Gum by the Solid Dispersion Technique
Article Menu

Article Versions

Export Article

Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Articles in this Issue were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence. Articles are hosted by MDPI on as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
Open AccessArticle
Sci. Pharm. 2014, 82(1), 193-206; (registering DOI)

Lectin-Grafted PLGA Microcarriers Loaded with Fluorescent Model Drugs: Characteristics, Release Profiles, and Cytoadhesion Studies

Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Althanstrasse 14, 1090, Vienna, Austria
Author to whom correspondence should be addressed.
Received: 10 December 2013 / Accepted: 8 February 2014 / Published: 8 February 2014
PDF [963 KB, uploaded 27 September 2016]


PLGA microparticles loaded with three different fluorescent model drugs, fluorescein sodium (hydrophilic), sulforhodamine (amphoteric), and boron-dipyrromethene (BODIPY® 493/503, lipophilic), were prepared by the solvent evaporation technique. Due to varying hydrophilicity, the diameters of the microparticles ranged between 4.1 and 4.7 μm. According to fluorimetric analysis, the loading varied from 0.06 to 2.25 μg of the model drug per mg PLGA. In terms of the release profile, the fluorescein sodium-entrapped formulation exhibited thermo-responsive release kinetics. In the case of sulforhodamine- and BODIPY® 493/503-loaded particles, almost no release was observed, neither at 4°C nor 37°C during the first 50 hours. Furthermore, to estimate the bioadhesive properties of such drug delivery systems, the surface of the loaded particles was grafted with wheat germ agglutinin by applying the carbodiimide method. Cytoadhesion studies with Caco-2 monolayers revealed an up to 1.9-fold and 3.6-fold increase in the bioadhesion of the lectin-functionalized, model drug-loaded particles as compared to the albumin- and non-grafted microcarriers, respectively. All in all, the results clearly indicated that the lipophilicity of the polymer matching that of the drug favored entrapment, whereas mismatching impeded loading into the PLGA-microparticles. Even in the case of low loading, these delivery systems might be useful for the fluorescent detections and microscopic imaging of cellular interactions due to their fluorescent properties and lack of dye leakage. Moreover, lectin grafting can mediate bioadhesive properties to such particulate drug carriers which could be a promising approach to improve drug delivery.
Keywords: Caco-2; Cytoadhesion; Microparticles; PLGA; Wheat Germ Agglutinin (WGA) Caco-2; Cytoadhesion; Microparticles; PLGA; Wheat Germ Agglutinin (WGA)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Share & Cite This Article

MDPI and ACS Style

WANG, X.-Y.; KOLLER, R.; WIRTH, M.; GABOR, F. Lectin-Grafted PLGA Microcarriers Loaded with Fluorescent Model Drugs: Characteristics, Release Profiles, and Cytoadhesion Studies. Sci. Pharm. 2014, 82, 193-206.

Show more citation formats Show less citations formats

Article Metrics

Article Access Statistics



[Return to top]
Sci. Pharm. EISSN 2218-0532 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top