Nanoparticulate-based drug delivery systems for small molecule anti-diabetic drugs: An emerging paradigm for effective therapy

Uppal, Siddharth; Italiya, Kishan S.; Chitkara, Deepak; Mittal, Anupama

doi:10.1016/j.actbio.2018.09.049

Cited by 68 publications

(33 citation statements)

References 170 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The oral route is by far the preferred route of drug administration for many dosages forms. However, many anti-diabetic drugs suffer from low bioavailability following oral administration especially BCS class III like metformin due to its high solubility and low permeability [17]. Therefore, microencapsulation…”

Section: Discussionmentioning

confidence: 99%

Potential of Sustained Release Microparticles of Metformin in Veterinary Medicine: An in Vivo Pharmacokinetic Study of Metformin Microparticles as Oral Sustained Release Formulation in Rabbits.

Bouriche¹,

Alonso-García²,

Cárceles-Rodríguez³

et al. 2020

Preprint

View full text Add to dashboard Cite

Background: Metformin hydrochloride a biguanide derivative has been widely used in the treatment of type 2 diabetes in humans. In veterinary medicine, metformin has been increasing his potential in different species as equids for insulin dysregulation, dogs and cats with diabetes. It is a highly soluble hydrophilic drug, shows incomplete absorption from the gastrointestinal tract and the absolute bioavailability is 40-60 % with a short biological half-life of 1.5-1.6 h in humans. In this study, to improve its efficacy a sustained-release microparticles of metformin was developed by loading within poly lactic acid (PLA) polymer followed by an in vivo pharmacokinetics study in rabbits. Results: Pharmacokinetic study in rabbits showed the sustained-release characteristic from the prepared microparticles with delayed time to reach maximum concentrations Tmax, decreased Cmax, increased Mean Residence Time (MRT) and half-life compared to the pure drug solution. Physicochemical characterization suggested that PLA and metformin hydrochloride interacted within the microparticles via hydrogen bonds and that the drug was transformed to an amorphous state. Conclusions: The The pharmacokinetics parameters resulted in delayed Tmax, increased MRT and t1/2, decreased Cmax of metformin from microparticles that show promise for prolonged/sustained release of metformin after oral administration in different animal species affected by insulin disorders. PLA microparticles provided sustained release of the drug, and these systems can be useful as drug carriers for hydrophilic drugs in long term disease treatment such as diabetes.

show abstract

Section: Discussionmentioning

confidence: 99%

Potential of Sustained Release Microparticles of Metformin in Veterinary Medicine: An in Vivo Pharmacokinetic Study of Metformin Microparticles as Oral Sustained Release Formulation in Rabbits.

Bouriche¹,

Alonso-García²,

Cárceles-Rodríguez³

et al. 2020

Preprint

View full text Add to dashboard Cite

show abstract

“…71 Oral nano delivery systems can not only protect antidiabetic phytocompounds from enzymatic and/or chemical degradation in GIT but also provide other benefits, such as avoidance of firstpass metabolism, improvement of pharmacokinetic and pharmacodynamic profile, fast onset of action, targeted drug delivery, sustained drug release, lower dose and dosing frequency, and fewer side effects. 2 (Table 1) (Figure 2), their impact on pharmacokinetic parameters, and their therapeutic effects.…”

Section: The Necessity Of Developing Antidiabetic Phytocompounds-loadmentioning

confidence: 99%

“…They can be a reservoir system in which drugs are enclosed in a cavity surrounded by polymeric membranes called nanocapsules or as a matrix system in which drugs are dispersed throughout particles called nanospheres ( Figure 2). 2 Polymers have attracted much attention in therapeutic applications because of the design flexibility based on functionalization, polymer diversity, and macromolecular synthesis methods. 117 According to the different materials used to construct them, polymer-based delivery systems can be divided into synthetic polymer NPs and inartificial polymer NPs.…”

Section: Polymeric Npsmentioning

confidence: 99%

See 1 more Smart Citation

<p>Oral Nano Drug Delivery Systems for the Treatment of Type 2 Diabetes Mellitus: An Available Administration Strategy for Antidiabetic Phytocompounds</p>

Nie¹,

Chen²,

Pang³

et al. 2020

IJN

View full text Add to dashboard Cite

In view of the worldwide serious health threat of type 2 diabetes mellitus (T2DM), natural sources of chemotherapies have been corroborated as the promising alternatives, with the excellent antidiabetic activities, bio-safety, and more cost-effective properties. However, their clinical application is somewhat limited, because of the poor solubility, instability in the gastrointestinal tract (GIT), low bioavailability, and so on. Nowadays, to develop nanoscaled systems has become a prominent strategy to improve the drug delivery of phytochemicals. In this review, we primarily summarized the intervention mechanisms of phytocompounds against T2DM and presented the recent advances in various nanosystems of antidiabetic phytocompounds. Selected nanosystems were grouped depending on their classification and structures, including polymeric NPs, lipid-based nanosystems, vesicular systems, inorganic nanocarriers, and so on. Based on this review, the state-of-the-art nanosystems for phytocompounds in T2DM treatment have been presented, suggesting the preponderance and potential of nanotechnologies.

show abstract

“…The drug-loaded microsphere depots can sustain drug release over time. Thus, drug-loaded microsphere depots can significantly reduce dosage frequency and improve drug efficacy via a single injection [3,4,5,6].…”

Section: Introductionmentioning

confidence: 99%

An Injectable Click-Crosslinked Hydrogel that Prolongs Dexamethasone Release from Dexamethasone-Loaded Microspheres

et al. 2019

View full text Add to dashboard Cite

Our purpose was to test whether a preparation of injectable formulations of dexamethasone (Dex)-loaded microspheres (Dex-Ms) mixed with click-crosslinked hyaluronic acid (Cx-HA) (or Pluronic (PH) for comparison) prolongs therapeutic levels of released Dex. Dex-Ms were prepared using a monoaxial-nozzle ultrasonic atomizer with an 85% yield of the Dex-Ms preparation, encapsulation efficiency of 80%, and average particle size of 57 μm. Cx-HA was prepared via a click reaction between transcyclooctene (TCO)-modified HA (TCO-HA) and tetrazine (TET)-modified HA (TET-HA). The injectable formulations (Dex-Ms/PH and Dex-Ms/Cx-HA) were fabricated as suspensions and became a Dex-Ms-loaded hydrogel drug depot after injection into the subcutaneous tissue of Sprague Dawley rats. Dex-Ms alone also formed a drug depot after injection. The Cx-HA hydrogel persisted in vivo for 28 days, but the PH hydrogel disappeared within six days, as evidenced by in vivo near-infrared fluorescence imaging. The in vitro and in vivo cumulative release of Dex by Dex-Ms/Cx-HA was much slower in the early days, followed by sustained release for 28 days, compared with Dex-Ms alone and Dex-Ms/PH. The reason was that the Cx-HA hydrogel acted as an external gel matrix for Dex-Ms, resulting in the retarded release of Dex from Dex-Ms. Therefore, we achieved significantly extended duration of a Dex release from an in vivo Dex-Ms-loaded hydrogel drug depot formed by Dex-Ms wrapped in an injectable click-crosslinked HA hydrogel in a minimally invasive manner. In conclusion, the Dex-Ms/Cx-HA drug depot described in this work showed excellent performance on extended in vivo delivery of Dex.

show abstract

Nanoparticulate-based drug delivery systems for small molecule anti-diabetic drugs: An emerging paradigm for effective therapy

Cited by 68 publications

References 170 publications

Potential of Sustained Release Microparticles of Metformin in Veterinary Medicine: An in Vivo Pharmacokinetic Study of Metformin Microparticles as Oral Sustained Release Formulation in Rabbits.

Potential of Sustained Release Microparticles of Metformin in Veterinary Medicine: An in Vivo Pharmacokinetic Study of Metformin Microparticles as Oral Sustained Release Formulation in Rabbits.

<p>Oral Nano Drug Delivery Systems for the Treatment of Type 2 Diabetes Mellitus: An Available Administration Strategy for Antidiabetic Phytocompounds</p>

An Injectable Click-Crosslinked Hydrogel that Prolongs Dexamethasone Release from Dexamethasone-Loaded Microspheres

Contact Info

Product

Resources

About