Nanoparticulate Drug Delivery Systems for Metformin Therapy

Metformin is the cornerstone of type 2 diabetes management and is increasingly recognised for anti-inflammatory and anticancer properties. Conventional oral administration, however, suffers from variable absorption, rapid clearance and gastrointestinal side effects. Nanoparticulate drug delivery systems seek to address these limitations by encapsulating metformin within carriers sized below 200 nm, thereby improving solubility, prolonging circulation time and enabling targeted release. Carriers range from biodegradable polymers and lipid vesicles to inorganic and hybrid nanomaterials, each tailored to tune release kinetics, enhance cellular uptake and reduce off-target effects. Polymeric nanoparticles often exploit poly(lactic-co-glycolic acid) matrices or chitosan coatings to achieve sustained release and mucoadhesion, while lipid-based vesicles offer biocompatibility and ease of surface functionalisation. Emerging platforms such as quantum-dot or graphene-based conjugates merge imaging and therapeutic functions. By refining particle size distribution, surface charge and drug-loading capacity, these systems hold promise for dose reduction, improved patient compliance and expanded therapeutic applications beyond glycaemic control into oncology and cardiovascular disease.

Research from Nature Portfolio

Recent studies have demonstrated the synthesis of a polymeric metformin conjugate that integrates both carrier and therapeutic functions. By linking metformin’s biguanide moieties to a cationic polymer backbone, researchers engineered nanoparticles capable of co-delivering small interfering RNA alongside intrinsic metformin activity. The resulting core–shell assemblies achieved efficient siRNA protection and release, activated AMP-activated protein kinase while inhibiting mTOR pathways, and exhibited enhanced tumour-suppressive efficacy in vivo. This dual-function nanoplatform exemplifies how metformin can be repurposed as both payload and carrier to potentiate combination therapies in oncology.

Nanoparticulate Drug Delivery Systems for Metformin Therapy publication trend

The graph below shows the total number of articles in nanoparticulate drug delivery systems for metformin therapy across all publications each year (not limited to Nature Index journals).

Technical terms

Nanoparticulate drug delivery system: A carrier system consisting of particles in the 1–200 nm range designed to transport and release therapeutic agents in a controlled manner.

Entrapment efficiency: The percentage of drug encapsulated within a carrier relative to the total drug used in formulation, indicating loading success.

Zeta potential: A measure of particle surface charge that predicts colloidal stability and interactions with biological membranes.

Poly(lactic-co-glycolic acid) (PLGA): A biodegradable copolymer frequently used to fabricate nanoparticles with tunable degradation and release profiles.

Graphene oxide quantum dot: A nanoscale fragment of graphene oxide with unique optical and surface characteristics, employed as a multifunctional drug carrier and imaging agent.

References

1. Emerging nanoparticulate drug delivery systems of metformin. Journal of Pharmaceutical Investigation (2020).
2. PolyMetformin combines carrier and anticancer activities for in vivo siRNA delivery. Nature Communications (2016).
3. Efficacy of pegylated Graphene oxide quantum dots as a nanoconjugate sustained release metformin delivery system in in vitro insulin resistance model. PLOS ONE (2024).
4. A PHYSIOCHEMICAL STUDY ON DRUG DELIVERY OF METFORMIN HCL-LOADED CS-PLGA NANOPARTICLES. International Journal of Applied Pharmaceutics (2023).