Spontaneous arrangement of a tumor targeting hyaluronic acid shell on irinotecan loaded PLGA nanoparticles
Authors: Assunta Borzacchiello
Marco Biondi
Simona Giarra
Giuseppe De Rosa
Stefania Zeppetelli
Laura Mayol
Luisa Russo
Carla Serri
Luigi Ambrosio
Journal: Carbohydrate Polymers (2016)
Discipline: CHEMISTRY
Keywords: CD44; Hyaluronic acid; Nanoparticle; PLGA; Poloxamer
Affiliations: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy., Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy; Dipartimento di Scienze del Farmaco e dei Prodotti per la Salute, Università degli Studi di Messina, Viale Annunziata, 98100 Messina, Italy., Institute for Polymers, Composites and Biomaterials, National Research Council, Mostra d'Oltremare Pad. 20, Viale J. F. Kennedy 54, 80125 Napoli, Italy., Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy; Interdisciplinary Research Centre on Biomaterials - CRIB, Università di Napoli Federico II, P.le Tecchio 80, Napoli, Italy., Institute for Polymers, Composites and Biomaterials, National Research Council, Mostra d'Oltremare Pad. 20, Viale J. F. Kennedy 54, 80125 Napoli, Italy. Electronic address: ., Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy; Interdisciplinary Research Centre on Biomaterials - CRIB, Università di Napoli Federico II, P.le Tecchio 80, Napoli, Italy. Electronic address: .

Abstract:  The arrangement of tumor targeting hyaluronic acid (HA) moieties on irinotecan (IRIN)-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) has been directed by means of a gradient of lipophilicity between the oil and water phases of the emulsion used to produce the NPs. PLGA constitutes the NP bulk while HA is superficially exposed, with amphiphilic poloxamers acting as a bridge between PLGA and HA. Differential scanning calorimetry, zeta potential analyses and ELISA tests were employed to support the hypothesis of polymer assembly in NP formulations. The presence of flexible HA chains on NP surface enhances NP size stability over time due to an increased electrostatic repulsion between NPs and a higher degree of hydration of the device surface. IRIN in vitro release kinetics can be sustained up to 7-13 days. In vitro biologic studies indicated that HA-containing NPs were more toxic than bare PLGA NPs against CD44-overexpressing breast carcinoma cells (HS578T), therefore indicating their ability to target CD44 receptor. 

Retracted: No

PubPeer comments:
 In this article, the nanoparticle size is surprisingly homogenous with extremely low variation in diameter (shown in Table 2). When the authors present electron microscopy data showing the size of the nanoparticles (Figure 4 and 5), which constitutes most of the raw data in this article, the results do not fit with the numbers presented in Table 2. The raw data indicates much more variation in the nanoparticle size. In addition the nanoparticles in the zoomed micrographs in Figure 4 and 5 do not correspond with the nanoparticle in the lower magnification micrographs. ![file] ![file] ,