Insights into Factors Affecting Ethylene-Vinyl Acetate Copolymer Crystallinity in Islatravir Implant

• DOI: 10.1021/acs.molpharmaceut.3c01198
• Publication Date: 2024-03-19T16:38:47Z
• Authors: Xiaolong Zhu; Ashish Punia; Daniel Skomski; Yongchao Su; C. Scott Shultz; Morgan B. Giles; Nathan D. Rudd; Nisha Raman; Athanas Koynov; Matthew S. Lamm
• Keywords: Ethylene-vinyl acetate; Vinyl acetate

Islatravir, a highly potent nucleoside reverse transcriptase translocation inhibitor (NRTTI) for the treatment of HIV, has great potential to be formulated as ethylene-vinyl acetate (EVA) copolymer-based implants via hot melt extrusion. The crystallinity EVA determines its physical and rheological properties may impact drug-eluting implant performance. Herein, we describe systematic analysis factors affecting in islatravir implants. Differential scanning calorimetry (DSC) on solid-state NMR revealed drug loading promoted crystallization, whereas BaSO4 had negligible crystallinity. sterilization through γ-irradiation appeared significantly surface characteristics Furthermore, DSC thin slices prepared with an ultramicrotome indicated that layer was more crystalline than core. These findings provide critical insights into crystallinity, mechanical properties, physicochemical polymer matrix extruded