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Article

PLGA-BMP-2 and PLA-17β-Estradiol Microspheres Reinforcing a Composite Hydrogel for Bone Regeneration in Osteoporosis

1
Department of Chemical Engineering and Pharmaceutical Technology, University of La Laguna, 38206 La Laguna, Spain
2
Institute of Biomedical Technologies (ITB), University of La Laguna, 38206 La Laguna, Spain
3
Department of Biochemistry, Microbiology, Cell Biology and Genetics, University of La Laguna, 38206 La Laguna, Spain
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2019, 11(12), 648; https://doi.org/10.3390/pharmaceutics11120648
Received: 23 October 2019 / Revised: 21 November 2019 / Accepted: 29 November 2019 / Published: 3 December 2019
(This article belongs to the Special Issue PLGA Based Drug Carrier and Pharmaceutical Applications)
The controlled release of active substances—bone morphogenetic protein 2 (BMP-2) and 17β-estradiol—is one of the main aspects to be taken into account to successfully regenerate a tissue defect. In this study, BMP-2- and 17β-estradiol-loaded microspheres were combined in a sandwich-like system formed by a hydrogel core composed of chitosan (CHT) collagen, 2-hidroxipropil γ-ciclodextrin (HP-γ-CD), nanoparticles of hydroxyapatite (nano-HAP), and an electrospun mesh shell prepared with two external electrospinning films for the regeneration of a critical bone defect in osteoporotic rats. Microspheres were made with poly-lactide-co-glycolide (PLGA) to encapsulate BMP-2, whereas the different formulations of 17β-estradiol were prepared with poly-lactic acid (PLA) and PLGA. The in vitro and in vivo BMP-2 delivered from the system fitted a biphasic profile. Although the in vivo burst effect was higher than in vitro the second phases (lasted up to 6 weeks) were parallel, the release rate ranged between 55 and 70 ng/day. The in vitro release kinetics of the 17β-estradiol dissolved in the polymeric matrix of the microspheres depended on the partition coefficient. The 17β-estradiol was slowly released from the core system using an aqueous release medium (Deff = 5.58·10−16 ± 9.81·10−17m2s−1) and very fast in MeOH-water (50:50). The hydrogel core system was injectable, and approximately 83% of the loaded dose is uniformly discharged through a 20G needle. The system placed in the defect was easily adapted to the defect shape and after 12 weeks approximately 50% of the defect was refilled by new tissue. None differences were observed between the osteoporotic and non-osteoporotic groups. Despite the role of 17β-estradiol on the bone remodeling process, the obtained results in this study suggest that the observed regeneration was only due to the controlled rate released of BMP-2 from the PLGA microspheres. View Full-Text
Keywords: BMP-2-microspheres; hydrogel system; 17-βestradiol release; bone regeneration; osteoporosis; poly-lactide-co-glycolide; polylactic acid BMP-2-microspheres; hydrogel system; 17-βestradiol release; bone regeneration; osteoporosis; poly-lactide-co-glycolide; polylactic acid
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MDPI and ACS Style

García-García, P.; Reyes, R.; Segredo-Morales, E.; Pérez-Herrero, E.; Delgado, A.; Évora, C. PLGA-BMP-2 and PLA-17β-Estradiol Microspheres Reinforcing a Composite Hydrogel for Bone Regeneration in Osteoporosis. Pharmaceutics 2019, 11, 648. https://doi.org/10.3390/pharmaceutics11120648

AMA Style

García-García P, Reyes R, Segredo-Morales E, Pérez-Herrero E, Delgado A, Évora C. PLGA-BMP-2 and PLA-17β-Estradiol Microspheres Reinforcing a Composite Hydrogel for Bone Regeneration in Osteoporosis. Pharmaceutics. 2019; 11(12):648. https://doi.org/10.3390/pharmaceutics11120648

Chicago/Turabian Style

García-García, Patricia, Ricardo Reyes, Elisabet Segredo-Morales, Edgar Pérez-Herrero, Araceli Delgado, and Carmen Évora. 2019. "PLGA-BMP-2 and PLA-17β-Estradiol Microspheres Reinforcing a Composite Hydrogel for Bone Regeneration in Osteoporosis" Pharmaceutics 11, no. 12: 648. https://doi.org/10.3390/pharmaceutics11120648

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