PLGA and PEG based porous microparticles as vehicles for pulmonary Somatropin delivery

Eur J Pharm Biopharm. 2023 Sep 1:S0939-6411(23)00230-8. doi: 10.1016/j.ejpb.2023.08.017. Online ahead of print.ABSTRACTBreakthrough advances in protein therapeutics and sustained release systems continue to fuel innovation in novel, non-invasive polymeric platforms for delivery of biologicals. Despite the bench potential and proof-of-concept work, market analysis still shows biologicals to be predominantly injections. Characterized by insufficient secretion of growth hormone by the pituitary gland, growth hormone deficiency (GHD) is a rare disorder. Currently, chronic somatropin (r-hGH) replacement therapy is only available as subcutaneous injections administered several times a week. We aim to prepare large, porous, biodegradable and aerodynamically light microparticles as tunable carriers for pulmonary r-hGH delivery. We developed a range of microparticles using PLGA 5050 1Awith sizes between 5 μm and 13 μm, densities lower than 0.4 g/cc and aerodynamic diameters lower than 6 μm. Polyethylene glycol's multitude of advantages - plasticizing PLGA, improving the biocompatibility of the system and preventing protein burst release - have been extensively studied, making it our excipient (pore-former) of choice. Drug loading was characterized at pH 4.0 (acidic), 5.3 (pI) and pH 7.2 (neutral) and was a result of an interplay of electrostatic and hydrophobic interactions between the polymer and somatropin. Considering the physicochemical interactions, we observed some pH depende...
Source: European Journal of Pharmaceutics and Biopharmaceutics - Category: Drugs & Pharmacology Authors: Source Type: research