ArticleThe AAPS journal2018
Reverse Engineering the 1-Month Lupron Depot®.
Article in The AAPS journal, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
18 citing papers in PubMed.
- Tumor-Targeted Delivery Therapy Based on PLGA Nanoparticles.Journal of functional biomaterials · 2026Review
- Redefining long-acting injectables: the emerging role of extracellular vesicles in sustained drug delivery.Drug delivery and translational research · 2026Review
- Effect of PLGA raw materials on in vitro and in vivo performance of drug-loaded microspheres.Drug delivery and translational research · 2025Article
- Patient-Centric Long-Acting Injectable and Implantable Platforms─An Industrial Perspective.Molecular pharmaceutics · 2024Review
- Antitumoral-Embedded Biopolymeric Spheres for Implantable Devices.Pharmaceutics · 2024Article
- Microstructure Formation and Characterization of Long-Acting Injectable Microspheres: The Gateway to Fully Controlled Drug Release Pattern.International journal of nanomedicine · 2024Review
- Overview of Antimicrobial Biodegradable Polyester-Based Formulations.International journal of molecular sciences · 2023Review
- Shape-specific microfabricated particles for biomedical applications: a review.Drug delivery and translational research · 2022Review
- Efficient aqueous remote loading of peptides in poly(lactic-co-glycolic acid).Nature communications · 2022Article
- Metal-HisTag coordination for remote loading of very small quantities of biomacromolecules into PLGA microspheres.Bioengineering & translational medicine · 2022Article
- Challenges and Complications of Poly(lactic-Pharmaceutics · 2022Review
- Article
- Development and characterization of composition-equivalent formulations to the Sandostatin LAR® by the solvent evaporation method.Drug delivery and translational research · 2022Article
- Changing the daily injection of glatiramer acetate to a monthly long acting product through designing polyester-based polymeric microspheres.BioImpacts : BI · 2022Article
- FDA's Poly (Lactic-Co-Glycolic Acid) Research Program and Regulatory Outcomes.The AAPS journal · 2021Review
- Key Factor Study for Generic Long-Acting PLGA Microspheres Based on a Reverse Engineering of VivitrolMolecules (Basel, Switzerland) · 2021Article
- Formulation composition, manufacturing process, and characterization of poly(lactide-co-glycolide) microparticles.Journal of controlled release : official journal of the Controlled Release Society · 2021Review
- Just how prevalent are peptide therapeutic products? A critical review.International journal of pharmaceutics · 2020Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors.
Funding
Abstract
The 1-month Lupron Depot® (LD) encapsulating water-soluble leuprolide in poly(lactic-co-glycolic acid) (PLGA) microspheres is a benchmark product upon which modern long-acting release products are often compared. Despite expiration of patent coverage, no generic product for the LD has been approved in the USA, likely due to the complexity of components and manufacturing processes involved in the product. Here, we describe the reverse engineering of the LD composition and important product attributes. Specific attributes analyzed for microspheres were as follows: leuprolide content by three methods; gelatin content, type, and molecular weight distribution; PLGA content, lactic acid/glycolic acid ratio, and molecular weight distribution; mannitol content; in vitro drug release; residual solvent and moisture content; particle size distribution and morphology; and glass transition temperature. For the diluent, composition, viscosity, and specific gravity were analyzed. Analyzed contents of the formulation and the determined PLGA characteristics matched well with the official numbers stated in the package insert and those found in literature, respectively. The gelatin was identified as type B consistent with ~ 300 bloom. The 11-μm volume-median microspheres in the LD slowly released the drug in vitro in a zero-order manner after ~ 23% initial burst release. Very low content of residual moisture (< 0.5%) and methylene chloride (< 1 ppm) in the product indicates in-water drying is capable of removing solvents to extremely low levels during manufacturing. The rigorous approach of reverse engineering described here may be useful for development of generic leuprolide-PLGA microspheres as well as other new and generic PLGA microsphere formulations.
Indexed as
Identifiers
30280294What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.