Gastroretentive Metformin Loaded Nanoparticles for the Effective Management of Type-2 Diabetes Mellitus

Abstract

Introduction: Metformin, an anti-diabetic drug, has low bioavailability and a short biological half-life. Thus, bioavailability enhancement and prolonged release of the drug are highly desirable. In this regard, we aimed to developed gastroretentive nanoparticles made of jackfruit seed starch (JFSS) loaded with metformin. Methods: The developed nanoparticles were optimized for various process variables and were further characterized. Nanoparticles exhibited good results with respect to particle size (244.3 to 612.4 nm), particle size distribution, shape, and drug entrapment efficiency (75.8 to 89.2 %) with sustained drug release for 24 h and a high buoyancy (89% for F7, formulation made of the highest concentration of Jackfruit seed starch prepared at 1000 RPM stirring speed). Results: The hypoglycemic potential of these nanoparticles was tested in the nicotinamide streptozocin induced diabetic model; there was a significant reduction in blood glucose level (50 % reduction from 4 - 8 h, p < 0.01) for a prolonged period of time (up to 24 h) in comparison to diabetic control and plain metformin solution. Conclusion: The outcome of the study suggested that the developed formulations are suitable for gastro-retentive delivery of Metformin in a controlled manner appropriate for a single administration per day.

An injectable vitreous substitute with sustained release of metformin for enhanced uveal melanoma immunotherapy

“…As metformin was proved to be an effective anti-tumor drug with a short half-life, we encapsulated metformin in IVS to prolong its release. 29–31 As shown in Fig. S8 and S9,† IVS-Met showed sustained release of metformin, maintaining its effective drug concentration in eyeballs.…”

“…27,28 However, the short elimination half-life of metformin has restricted its antitumor effects. [29][30][31] In our study, the injectable vitreous substitute with sustained metformin release ability (IVS-Met) prolonged the action of metformin and achieved an excellent long-term anti-tumor effect. Apart from direct tumor attack, IVS-Met could reduce the proportion of pro-tumor M2 phenotype tumor-associated macrophages (M2 TAMs) and induce pro-inflammatory M1 phenotype TAMs (M1 TAMs), therefore reversing the immunosuppressive TME and eliciting robust anti-tumor immune responses.…”

Hyaluronic acid-graphene oxide quantum dots nanoconjugate as dual purpose drug delivery and therapeutic agent in meta-inflammation

“…Numerous earlier researches have examined various nano formulations for metformin delivery in type 2 diabetes [ 75 – 77 ]. Since metformin exhibits poor bioavailability and necessitates greater doses, the majority of studies solely employ the nanoformulation as a carrier with a primary focus on the sustained release of the medication [ 78 – 80 ]. In our investigation, loading metformin onto the GOQD-HA increased the drug's targetability and bioavailability, which was demonstrated by the fact that lower dosages were needed to achieve the same effects as free metformin.…”

Research progress of starch from characteristic tropical crops

“…通过改性可以改变淀粉的消化特性, 如通过挤压膨化 [156] 提高淀粉消化性, 通过湿热处理 [302] 、退火处理 [303] 提高抗性淀粉含量. 菠萝蜜淀粉以原 淀粉 [304] 或交联改性淀粉 [305] 的形式在药品中用作赋形剂和崩解剂, 或者经过纳米化对药物进行包封 [306] . 菠 萝蜜淀粉膜材料主要作为食品保鲜涂层 [307,308] 和生物降解塑料 [309][310][311] 应用, 菠萝蜜淀粉膜材料的主要通过 共混技术和浇铸技术制得.…”