SUSTAINED RELEASE GEL 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 solution characteristics • Application: sustained delivery of small molecule, peptide & protein Applied as suspension • 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 Solvent(s) diffuses & polymer polymer solidifies at site
Polymer degrades, Drug releases drug releases over time
Formulation Screening Gel Formulation - Dosage Form Various Gel Systems for Weekly Delivery
Suspension Solution Gel Gel Formulation Formulation
Attribute Solution Suspension Need suitable solubilizing API Solubility 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 solid 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 mixtures 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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