John Garner

PLGA-PEG-PLGA from PolySciTech used for localized propranolol delivery system

Blog Post created by John Garner on Nov 1, 2017

PolyVivo AK016 Hemangioma treatement propranolol polyscitech.jpg

Hemangioma (red or purple colored birthmarks) is a benign childhood tumor generated by excessive growth of blood vessels. Although external hemangioma’s typically only affect aesthetics, the growth of internal hemangiomas, especially near liver, brain, or other critical organs, can cause severe pain and morbidity.  Treatment options include corticosteroids and beta-blockers, however applying such treatments to infants and children throughout the whole body in a systemic fashion can create problems with controlling the dose and side-effects. Recently, researchers at Henan Provincial People’s Hospital and the Second Military Medical University (China) used PLGA-PEG-PLGA (PolyVivo AK016) from PolySciTech (www.polyscitech.com) to generate microparticles as part of a local propranolol delivery system. These particles were found to be effective at delivering propranolol (a beta blocker) locally without requiring a large systemic dose. This research holds promise for treating a variety of conditions where excessive angiogenesis is a problem. Read more: Guo, Xiaonan, Xiaoshuang Zhu, Dakan Liu, Yubin Gong, Jing Sun, and Changxian Dong. "Continuous delivery of propranolol from liposomes-in-microspheres significantly inhibits infantile hemangioma growth." International Journal of Nanomedicine 12 (2017): 6923. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5609781/

 

“Purpose: To reduce the adverse effects and high frequency of administration of propranolol to treat infantile hemangioma, we first utilized propranolol-loaded liposomes-in-microsphere (PLIM) as a novel topical release system to realize sustained release of propranolol. Methods: PLIM was developed from encapsulating propranolol-loaded liposomes (PLs) in microspheres made of poly(lactic-co-glycolic acid)-b-poly(ethylene glycol)-b-poly(lactic-co-glycolic acid) copolymers (PLGA-PEG-PLGA). The release profile of propranolol from PLIM was evaluated, and its biological activity was investigated in vitro using proliferation assays on hemangioma stem cells (HemSCs). Tumor inhibition was studied in nude mice bearing human subcutaneous infantile hemangioma. Results: The microspheres were of desired particle size (~77.8 μm) and drug encapsulation efficiency (~23.9%) and achieved sustained drug release for 40 days. PLIM exerted efficient inhibition of the proliferation of HemSCs and significantly reduced the expression of two angiogenesis factors (vascular endothelial growth factor-A [VEGF-A] and basic fibroblast growth factor [bFGF]) in HemSCs. Notably, the therapeutic effect of PLIM in hemangioma was superior to that of propranolol and PL in vivo, as reflected by significantly reduced hemangioma volume, weight, and microvessel density. The mean hemangioma weight of the PLIM-treated group was significantly lower than that of other groups (saline =0.28 g, propranolol =0.21 g, PL =0.13 g, PLIM =0.03 g; PLIM vs saline: P<0.001, PLIM vs propranolol: P<0.001, PLIM vs PL: P<0.001). The mean microvessel density of the PLIM-treated group was significantly lower than that of other groups (saline =40 vessels/mm2, propranolol =31 vessels/mm2, PL =25 vessels/mm2, PLIM =11 vessels/mm2; PLIM vs saline: P<0.001, PLIM vs propranolol: P<0.01, PLIM vs PL: P<0.05). Conclusion: Our findings show that PLIM is a very promising approach to locally and efficiently deliver propranolol to the hemangioma site leading to a significant inhibition of infantile hemangioma. Keywords: propranolol, liposomes, microsphere, controlled release, hemangioma”

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