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SUSTAINED RELEASE FORMULATION

Release Mechanism PLGA - poly(lactic-co-glycolic acid) • Monomer: lactic acid (LA) and glycolic acid (GA) Gel Formulation • Amorphous, biocompatible andbiodegradable polymer Excipient + Drug (Tg: 40-60 C) • Long clinical experience, favorable degradation in polymer characteristics • Application: sustained delivery of small molecule, peptide & protein Applied as • Degradation: hydrolysis of its ester linkages in the presence or solution of water Gel depot forms • Degradation half-life: determined by molecular weight, the ratio of lactic acid to glycolic acid and end group of (s) diffuses & polymer polymer solidifies at site

Polymer degrades, Drug releases drug releases over time

Formulation Screening Gel Formulation - Various Gel Systems for Weekly Delivery

Suspension Solution Gel Gel Formulation Formulation

Attribute Solution Suspension Need suitable solubilizing API NA agent API Particle Size Control & maintain PSD during NA (PSD) mfg & storage API Chemical Generally less stable in the Generally more stable in the Stability solution form API Physical Need suitable suspending NA Stability agent and avoid aggregation Larger dose volume due to Lower dose volume may Dose Volume solubility limitation require bigger needle Syringeablity Relatively smaller needle Relatively bigger needle Relatively higher initial Release Relatively lower initial burst burst Note: Standard mfg process Control & maintain PSD during SAIB gel contains 6% API loading Manufacturing DP can be sterilized by Aseptic mfg. DP cannot be PLGA gel contains 10% API loading with various solvent filtration filtered Autogel contains 30% API loading

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Formulation Screening Syringeability for PLGA Gel PLGA Gel for ≥ 3M Delivery Acceptable Break Loose Force

Break Loose Sample Needle Gauge Force (N) DDE Data: Break loose force 21G 1” 5.93 for PLGA Gel PLGA Gel-1 23G 1” UTW 6.12 Systems provide 25G 5/8” UTW 8.85 21G 1” 7.96 IVR in pH 7.4 at ≥ 3M Delivery PLGA Gel-2 23G 1” UTW 13.9 37°C, 50 rpm 25G 5/8” UTW 21.81 21G 1” 21.53 PLGA Gel-3 23G 1” UTW 41.71 25G 5/8” UTW ˃ 60 Plunger moving speed: 2 mm/sec Record force when dispensing 200 uL formulation with a 1 mL BD plastic Note: all formulations contain syringe Plunger moving 10% API loading direction

Single Dose in Rat, Gliding force Exposure ≥ 3M Acceptable Burst

DDE Proprietary Formulation PLGA Microsphere Reduced Initial Burst Various PLGA MW & Excipients Single Dose in Rat for Weekly Delivery

IVR in pH 7.4 at 37°C, 50 rpm

DDE Proprietary Gel IVR in pH 7.4 at systems showed 37°C, 50 rpm relatively slower release

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