Empagliflozin containing chitosan-alginate nanoparticles in orodispersible film: preparation, characterization, pharmacokinetic evaluation and its<i>in-vitro</i>anticancer activity

Suhani, Sinha; Sonali,; Garg, Vandana; Thapa, Sonia; Singh, Shashank; Chauhan, Mahima; Dutt, Rohit; Singh, Rahul Pratap

doi:10.1080/03639045.2022.2108829

Cited by 11 publications

(5 citation statements)

References 44 publications

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“…Research has shown a remarkable 11-fold increase in the in vitro drug release from polymeric films embedded with nanoparticles in comparison to the pure drug [ 139 ]. Other researchers have reported identical improvements in ex vivo permeation, emphasizing the substantial promise of using nanoparticle-loaded ODFs for the delivery of poorly soluble compounds [ 140 , 141 ]. In a recent study, scientists employed the Box–Behnken method to design and fabricate ODFs loaded with ketoprofen nanoparticles [ 142 ].…”

Section: Nanoparticle-embedded Odfsmentioning

confidence: 94%

Orodispersible Films: Current Innovations and Emerging Trends

Jacob,

Boddu,

Bhandare

et al. 2023

Pharmaceutics

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Orodispersible films (ODFs) are thin, mechanically strong, and flexible polymeric films that are designed to dissolve or disintegrate rapidly in the oral cavity for local and/or systemic drug delivery. This review examines various aspects of ODFs and their potential as a drug delivery system. Recent advancements, including the detailed exploration of formulation components, such as polymers and plasticizers, are briefed. The review highlights the versatility of preparation methods, particularly the solvent-casting production process, and novel 3D printing techniques that bring inherent flexibility. Three-dimensional printing technology not only diversifies active compounds but also enables a multilayer approach, effectively segregating incompatible drugs. The integration of nanoparticles into ODF formulations marks a significant breakthrough, thus enhancing the efficiency of oral drug delivery and broadening the scope of the drugs amenable to this route. This review also sheds light on the diverse in vitro evaluation methods utilized to characterize ODFs, ongoing clinical trials, approved marketed products, and recent patents, providing a comprehensive outlook of the evolving landscape of orodispersible drug delivery. Current patient-centric approaches involve developing ODFs with patient-friendly attributes, such as improved taste masking, ease of administration, and enhanced patient compliance, along with the personalization of ODF formulations to meet individual patient needs. Investigating novel functional excipients with the potential to enhance the permeation of high-molecular-weight polar drugs, fragile proteins, and oligonucleotides is crucial for rapid progress in the advancing domain of orodispersible drug delivery.

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Section: Nanoparticle-embedded Odfsmentioning

confidence: 94%

Orodispersible Films: Current Innovations and Emerging Trends

Jacob,

Boddu,

Bhandare

et al. 2023

Pharmaceutics

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“…The FTIR spectra of crystalline DMF showed 1672 cm −1 for the C=C stretching vibration, 1719 and 3430 cm −1 for the C=O stretching vibration, 1160 cm −1 for the C−O stretching vibration, and 670-890 cm −1 and 2850-3080 cm −1 for the C−H bending vibration. These peaks were not found in either the 5% w/w DMF-HPMC(AS) physical mixture or the melt extruded solid dispersion containing 5% DMF [60] (Figure S2b). For comparison, the FTIR of pure polymers has been shown in Figure S2c.…”

Section: Pxrd and Ftirmentioning

confidence: 99%

Molecular Interactions between APIs and Enteric Polymeric Excipients in Solid Dispersion: Insights from Molecular Simulations and Experiments

2023

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Solid dispersion of poorly soluble APIs is known to be a promising strategy to improve dissolution and oral bioavailability. To facilitate the development and commercialization of a successful solid dispersion formulation, understanding of intermolecular interactions between APIs and polymeric carriers is essential. In this work, first, we assessed the molecular interactions between various delayed-release APIs and polymeric excipients using molecular dynamics (MD) simulations, and then we formulated API solid dispersions using a hot melt extrusion (HME) technique. To assess the potential API–polymer pairs, three quantities were evaluated: (a) interaction energy between API and polymer [electrostatic (Ecoul), Lenard-Jones (ELJ), and total (Etotal)], (b) energy ratio (API–polymer/API–API), and (c) hydrogen bonding between API and polymer. The Etotal quantities corresponding to the best pairs: NPX-Eudragit L100, NaDLO–HPMC(P), DMF–HPMC(AS) and OPZ–HPMC(AS) were −143.38, −348.04, −110.42, and −269.43 kJ/mol, respectively. Using a HME experimental technique, few API–polymer pairs were successfully extruded. These extruded solid forms did not release APIs in a simulated gastric fluid (SGF) pH 1.2 environment but released them in a simulated intestinal fluid (SIF) pH 6.8 environment. The study demonstrates the compatibility between APIs and excipients, and finally suggests a potential polymeric excipient for each delayed-release API, which could facilitate the development of the solid dispersion of poorly soluble APIs for dissolution and bioavailability enhancement.

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“…These findings highlight the potential of empagliflozin as an effective inhibitor of lung cancer cells. In addition, Sinha et al [ 70 ] prepared an orally dispersible film agent with chitosan-sodium alginate nanoparticles loaded with empagliflozin. Studies demonstrated that empagliflozin chitosan-sodium alginate nanoparticles had a relatively high bioavailability in the Wistar rat model and were 2.5 times more cytotoxic to A549 lung cancer cells than free empagliflozin [ 70 ].…”

Section: Empagliflozin and Cancermentioning

confidence: 99%

“…In addition, Sinha et al [ 70 ] prepared an orally dispersible film agent with chitosan-sodium alginate nanoparticles loaded with empagliflozin. Studies demonstrated that empagliflozin chitosan-sodium alginate nanoparticles had a relatively high bioavailability in the Wistar rat model and were 2.5 times more cytotoxic to A549 lung cancer cells than free empagliflozin [ 70 ]. Treatment of A549 lung cancer cells with the oral dispersion film agent of chitosan-sodium alginate nanoparticles loaded with empagliflozin resulted in a significantly lower IC 50 concentration of 69.24 µg/ml compared to treatment with free empagliflozin, suggesting the potential of this dispersion film agent as a more effective treatment option [ 70 ].…”

Section: Empagliflozin and Cancermentioning

confidence: 99%

“…Studies demonstrated that empagliflozin chitosan-sodium alginate nanoparticles had a relatively high bioavailability in the Wistar rat model and were 2.5 times more cytotoxic to A549 lung cancer cells than free empagliflozin [ 70 ]. Treatment of A549 lung cancer cells with the oral dispersion film agent of chitosan-sodium alginate nanoparticles loaded with empagliflozin resulted in a significantly lower IC 50 concentration of 69.24 µg/ml compared to treatment with free empagliflozin, suggesting the potential of this dispersion film agent as a more effective treatment option [ 70 ]. The mechanism of action of empagliflozin in treating lung cancer remains unclear, but it has been shown that SGLT2 is a target of action in several cancers as well as diabetes [ 71 ].…”

Section: Empagliflozin and Cancermentioning

confidence: 99%

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Empagliflozin: a potential anticancer drug

Wang

Xie

et al. 2023

Discov Onc

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Empagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor, is a highly effective and well-tolerated antidiabetic drug. In addition to hypoglycemic effects, empagliflozin has many other effects, such as being hypotensive and cardioprotective. It also has anti-inflammatory and antioxidative stress effects in diabetic nephropathy. Several studies have shown that empagliflozin has anticancer effects. SGLT2 is expressed in a variety of cancer cell lines. The SGLT2 inhibitor empagliflozin has significant inhibitory effects on certain types of tumor cells, such as inhibition of proliferation, migration and induction of apoptosis. In conclusion, empagliflozin has promising applications in cancer therapy as a drug for the treatment of diabetes and heart failure. This article provides a brief review of the anticancer effects of empagliflozin.

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Empagliflozin containing chitosan-alginate nanoparticles in orodispersible film: preparation, characterization, pharmacokinetic evaluation and itsin-vitroanticancer activity

Cited by 11 publications

References 44 publications

Orodispersible Films: Current Innovations and Emerging Trends

Orodispersible Films: Current Innovations and Emerging Trends

Molecular Interactions between APIs and Enteric Polymeric Excipients in Solid Dispersion: Insights from Molecular Simulations and Experiments

Empagliflozin: a potential anticancer drug

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