Abstract
In this work, we aimed to determine the role of the mechanical, structural, and thermal properties of poly(l-lactide-co-glycolide-co-trimethylene carbonate) (P(l-LA:GA:TMC)) with shape memory in the formulation of implantable and biodegradable rods with aripiprazole (ARP). Hot melt extrusion (HME) and electron beam (EB) irradiation were applied in the formulation process of blank rods and rods with ARP. Rod degradation was carried out in a PBS solution. HPLC; NMR; DSC; compression and tensile tests; molecular weight (Mn); water uptake (WU); and weight loss (WL) analyses; and SEM were used in this study. HME and EB irradiation did not influence the structure of ARP. The mechanical tests indicated that the rods may be safely implanted using a pre-filled syringe. During degradation, no unfavorable changes in terpolymer content were observed. A decrease in the glass transition temperature and the Mn, and an increase in the WU and the WL were revealed. The loading of ARP and EB irradiation induced earlier pore formation and more intense WU and WL changes. ARP was released in a tri-phasic model with the lag phase; therefore, the proposed formulation may be administered as a delayed-release system. EB irradiation was found to accelerate ARP release.
Highlights
Aripiprazole (ARP) is an atypical antipsychotic with a unique receptor-binding profile
In this study implantable and biodegradable rods based on poly(L-lactide-co-glycolide-co-trimethylene carbonate) (P(L-LA:GA:TMC)) with ARP (P(L-LA:GA:TMC) rod-ARP) administered with a pre-filled syringe were developed as an alternative to the known solutions
Hot melt extrusion (HME) and electron beam (EB) irradiation were applied in the formulation process of
Summary
Aripiprazole (ARP) is an atypical antipsychotic with a unique receptor-binding profile. ARP in poly(caprolactone) nanoparticles [3], poly(lactide-coglycolide) (PLGA) microparticles [4,5], polylactide microparticles [6], and PLGA implants in situ [7] have been proposed. Small formulations such as microparticles are administered as aqueous suspensions, which may cause pain and cannot be removed if side effects appear. It was noted that P(L-LA:GA:TMC), which has similar structural properties, was able to move from a temporarily fixed shape back to its original permanent shape upon exposure to a thermal stimulus [8], which can be a significant advantage in administration This feature may reduce invasiveness because of the smaller diameter and greater length of the formulation before implantation, as well as its greater diameter and smaller length after implantation, as has been discussed previously [8,9]
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