Next Generation Drug Delivery Systems


Next Generation Drug Delivery Systems

 

Selected FDA-Approved PLGA-Based Long-Acting Drug Products

PLGA and closely related PLG polymers have been used in several FDA-approved long-acting injectable and localized drug-delivery products. These formulations demonstrate the versatility of biodegradable polymer technology for weekly, monthly, multi-month and site-specific drug release.

The following table presents selected examples for technical and educational reference.

FDA-Approved Product

Active Pharmaceutical Ingredient

PLGA-Based Delivery Format

Approved Application

Labelled Administration Pattern

LUPRON DEPOT – 1 Month

Leuprolide acetate

Lyophilized microspheres containing a biodegradable copolymer of lactic and glycolic acids

Treatment of advanced prostate cancer

Intramuscular administration every four weeks

SANDOSTATIN LAR DEPOT

Octreotide acetate

Biodegradable glucose-star PLGA microspheres

Acromegaly and symptoms associated with certain carcinoid tumours and VIPomas

Intramuscular administration every four weeks

RISPERDAL CONSTA

Risperidone

Risperidone encapsulated in 75:25 polylactide-co-glycolide microspheres

Schizophrenia and maintenance treatment of Bipolar I Disorder

Intramuscular administration every two weeks

VIVITROL

Naltrexone

Extended-release PLG microsphere formulation

Alcohol dependence and prevention of relapse to opioid dependence following detoxification

Deep intramuscular administration every four weeks or once monthly

TRELSTAR

Triptorelin pamoate

Sterile, lyophilized PLGA biodegradable microgranules

Treatment of advanced prostate cancer

Intramuscular administration every 4, 12 or 24 weeks, depending on strength

BYDUREON BCISE

Exenatide

Extended-release microspheres containing 50:50 poly(D,L-lactide-co-glycolide)

Improvement of glycaemic control in patients with Type 2 diabetes mellitus, as specified in the approved label

Subcutaneous administration once every seven days

ZILRETTA

Triamcinolone acetonide

75:25 PLGA microspheres for localized extended release

Management of osteoarthritis pain of the knee

Single intra-articular injection according to the approved label

SIGNIFOR LAR

Pasireotide pamoate

Active ingredient distributed within biodegradable PLGA microspheres

Treatment of acromegaly and Cushing’s disease in specified patient groups

Intramuscular administration once every four weeks

What These Products Demonstrate

These FDA-approved products illustrate that there is no universal PLGA grade for every sustained-release formulation. The appropriate polymer must be selected according to the active ingredient, intended route of administration, desired release period and manufacturing process.

Critical polymer attributes may include:

·       Lactide-to-glycolide ratio

·       Molecular weight and molecular-weight distribution

·       Inherent viscosity

·       Acid or ester end group

·       Linear, branched or glucose-initiated architecture

·       Polymer degradation behaviour

·       API–polymer interaction

·       Microsphere particle size and morphology

·       Residual monomer and residual solvent levels

FDA product-specific guidance for complex PLGA formulations may require comparative evaluation of polymer composition, molecular weight, molecular-weight distribution, architecture and other physicochemical characteristics during generic-product development.

PLGA Polymer Selection Support from Nomisma Healthcare

Nomisma Healthcare supports pharmaceutical formulators with high-purity PLGA polymers for microspheres, long-acting injectables and controlled-release drug-delivery systems.

Our portfolio includes multiple lactide-to-glycolide ratios, molecular-weight ranges, inherent viscosities and end-group options. Customized PLGA polymers can also be developed according to the required formulation process and target drug-release profile.

Our technical and analytical capabilities support:

·       Selection of suitable PLGA grades

·       Customized molecular-weight development

·       Acid-, ester- and glucose-initiated polymers

·       Polymer composition and end-group analysis

·       Molecular-weight distribution testing

·       Reference-product polymer characterization

·       Microsphere morphology and particle-size evaluation

·       Residual monomer, solvent and moisture testing

Discuss your PLGA microsphere project with the Nomisma Healthcare technical team to identify a suitable polymer for your formulation-development requirements.

Regulatory and Accuracy Notice

The products listed above are included only as publicly available examples of FDA-approved finished drug products that use PLGA, PLG or related biodegradable polymer-delivery technology.

The information does not constitute medical or prescribing advice and should not replace the current FDA-approved prescribing information.

The listing does not imply that Nomisma Healthcare manufactures or supplies the polymer used in these branded products. FDA approval of a finished drug product does not represent FDA approval, certification or endorsement of Nomisma Healthcare or any specific excipient supplier.

All trademarks and brand names belong to their respective owners.