Structural changes on polymeric nanoparticles induced by hydrophobic drug entrapment

Author(s)

Jager, Alessandro ^[1] ; Jager, Eliezer ^[1] ; Giacomelli, Fernando Carlos ^[2] ; Nallet, Frederic ^[3] ; Steinhart, Milos ^[1] ; Putaux, Jean-Luc ^{[4, 5]} ; Konefal, Rafal ^[1] ; Spevacek, Jiri ^[1] ; Ulbrich, Karel ^[1] ; Stepanek, Petr ^[1]

Affiliation

^[1] Inst Macromol Chem, Heyrovsky Sq 2, Prague 16206 6 - Czech Republic

^[2] Univ Fed ABC, Ctr Ciencias Nat & Humanas, BR-09210170 Santo Andre - Brazil

^[3] Univ Bordeaux, CNRS, Ctr Rech Paul Pascal, 115 Ave Schweitzer, F-33600 Pessac - France

^[4] CNRS, CERMAV, F-38000 Grenoble - France

^[5] Univ Grenoble Alpes, Ctr Rech Macromol Vegetales CERMAV, F-38000 Grenoble - France

• Document type: Journal article
• Source: COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS; v. 538, p. 238-249, FEB 5 2018.
• Web of Science Citations: 7

Abstract

The potential use of polyester polymeric nanoparticles (NPs) as drug nanocarriers is well-documented. Nevertheless, structural changes due to hydrophobic drug loading and release have been rarely explored. Herein, we have used static and dynamic light scattering (SDLS), small-angle X-ray scattering (SAXS), transmission electron microscopy (TEM) and cryo-TEM to probe how the entrapment of a hydrophobic drug molecule changes the nanoparticles feature. The presence of the hydrophobic drug molecule modifies the inner structure of the NPs. The polymeric assemblies are characterized by differences in their densities (similar to 0.06 g cm(-3) for poly(D, L-lactide) -PLA or poly(D, L-lactide-co-glycolide - PLGA) and 0.46 g cm(-3) for poly{[}(butylene succinate)-co-(butylene dilinoleate)] - PBSBDL). They are thus water swollen in the drug-free condition. The NPs were further prepared by using the same polyesters and given amounts of the poorly water-soluble drug paclitaxel (PTX). The density (d(NP)), R-G (radius of gyration), R-H (hydrodynamic radius), R-G/R-H and R (contrast radius) have been monitored as a function of the amount of drug loaded. The drug entrapment increased the size of PLA and PLGA NPs. On the other hand, it also promoted the shrinkage of PBSBDL NPs. These observations revealed that changes in the inner structure of soft nanoparticles caused by drug loading is not straightforward and it mainly depends on the strength of van der Waals interactions between the polyester core and the probe which is connected to their chemical composition and hydrophobicity. These findings are crucial to understand the key physicochemical parameters involved in the interactions between drug and polymer that affects the final particle structure and influence its loading, release and degradation. (AU)

• FAPESP's process: 12/14087-8 - Development of size-tuned polymeric nanoparticles and evaluation of the interaction with biological environments
• Grantee: Fernando Carlos Giacomelli
• Support Opportunities: Regular Research Grants