Enhanced bioavailability and antihypertensive activity of nisoldipine loaded nanoemulsion: optimization, cytotoxicity and uptake across Caco-2 cell line, pharmacokinetic and pharmacodynamic studies

Mundada, Veenu P; Patel, Manthan; Mundada, Piyush K; Sawant, Krutika

doi:10.1080/03639045.2020.1724128

Cited by 16 publications

(5 citation statements)

References 39 publications

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“…The cell nuclei were stained with DAPI. The cellular uptake was examined using CLSM 510 Meta (Olympus, FV3000, Tokyo, Japan) with an oil immersion objective (40×) [ 43 ].…”

Section: Methodsmentioning

confidence: 99%

Microemulsion Delivery System Improves Cellular Uptake of Genipin and Its Protective Effect against Aβ1-42-Induced PC12 Cell Cytotoxicity

Zheng

et al. 2022

Pharmaceutics

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Genipin has attracted much attention for its hepatoprotective, anti-inflammatory, and neuroprotection activities. However, poor water solubility and active chemical properties limit its application in food and pharmaceutical industries. This article aimed to develop a lipid-based microemulsion delivery system to improve the stability and bioavailability of genipin. The excipients for a genipin microemulsion (GME) preparation were screened and a pseudo-ternary phase diagram was established. The droplet size (DS), zeta potential (ZP), polydispersity index (PDI), physical and simulated gastrointestinal digestion stability, and in vitro drug release properties were characterized. Finally, the effect of the microemulsion on its cellular uptake by Caco-2 cells and the protective effect on PC12 cells were investigated. The prepared GME had a transparent appearance with a DS of 16.17 ± 0.27 nm, ZP of −8.11 ± 0.77 mV, and PDI of 0.183 ± 0.013. It exhibited good temperature, pH, ionic strength, and simulated gastrointestinal digestion stability. The in vitro release and cellular uptake data showed that the GME had a lower release rate and better bioavailability compared with that of free genipin. Interestingly, the GME showed a significantly better protective effect against amyloid-β (Aβ1-42)-induced PC12 cell cytotoxicity than that of the unencapsulated genipin. These findings suggest that the lipid-based microemulsion delivery system could serve as a promising approach to improve the application of genipin.

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“…The cell nuclei were stained with DAPI. The cellular uptake was examined using CLSM 510 Meta (Olympus, FV3000, Tokyo, Japan) with an oil immersion objective (40×) [ 43 ].…”

Section: Methodsmentioning

confidence: 99%

Microemulsion Delivery System Improves Cellular Uptake of Genipin and Its Protective Effect against Aβ1-42-Induced PC12 Cell Cytotoxicity

Zheng

et al. 2022

Pharmaceutics

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“…A visual inspection was utilized to evaluate the consistency of the optimized TH-NEG within a transparent glass vessel [25]. The pH measurement was conducted using a digital pH meter (HI 98107, Hanna Instruments, Navi Mumba, India) equipped with a glass microelectrode.…”

Section: Homogeneity and Phmentioning

confidence: 99%

Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis

Phagna,

Badhwar,

Singh

et al. 2023

Gels

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Dermatophytosis, the most prevalent fungal infection, is witnessing a rising incidence annually. To address this challenge, we developed a terbinafine-loaded oil-in-water nanoemulsion (TH-NE) through the aqueous microtitration method. The formulation comprised olive oil (oil phase), Span 80 (surfactant), and propylene glycol (co-surfactant). Pseudo-phase ternary diagrams and thermodynamic studies underscored the stability of TH-NE. Employing the Box–Behnken design (BBD), we optimized TH-NE, which resulted in a remarkable particle size of 28.07 nm ± 0.5, a low polydispersity index (PDI) of 0.1922 ± 0.1, and a substantial negative zeta potential of −41.87 mV ± 1. Subsequently, TH-NE was integrated into a 1.5% carbopol matrix, yielding a nanoemulgel (TH-NEG). Texture analysis of TH-NEG demonstrated a firmness of 168.00 g, a consistency of 229.81 g/s, negative cohesiveness (−83.36 g), and a work of cohesion at −107.02 g/s. In vitro drug release studies revealed an initial burst effect followed by sustained release, with TH-NEG achieving an impressive 88% release over 48 h, outperforming TH-NE (74%) and the marketed formulation (66%). Ex vivo release studies mirrored these results, with TH-NEG (86%) and TH-NE (71%) showcasing sustained drug release in comparison to the marketed formulation (67%). Confocal microscopy illustrated that TH-NEG and TH-NE penetrated to depths of 30 µm and 25 µm, respectively, into the epidermal layer. Furthermore, dermatokinetic studies highlighted the enhanced drug penetration of TH-NEG compared to TH-NE through mouse skin. In summary, our study establishes TH-NEG as a promising carrier for terbinafine in treating dermatophytosis, offering improved drug delivery and sustained release potential.

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“…Additionally, red ginger nanoemulsion therapy resulted in a 10.80% reduction in the level of ACE [ 88 ]. In a research study by Mundada et al, it was found that nisoldipine nanoemulsion had a significant reduction in systolic blood pressure from 187.31 ± 18.02 mmHg to 139.68 ± 13.12 mmHg and diastolic blood pressure from 122.36 ± 12.01 mmHg to 101.84 ± 10.28 mmHg [ 89 ]. In a research study by Gorain et al, it was observed that systolic blood pressure (115.71 ± 4.800 mmHg) was reduced after 1 hour of administration of Olmesartan nanoemulsion and was controlled up to 12 hours after administration (120.12 ± 5.724 mmHg).…”

Section: Nanoemulsion As Drug Delivery Systemmentioning

confidence: 99%

A Revolutionary Blueprint for Mitigation of Hypertension via Nanoemulsion

Kumar

Virmani

Pathak

2022

BioMed Research International

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Hypertension is one of the most important causes of mortality, affecting the health status of the patient. At the same time, hypertension causes a huge health and economic burden on the whole world. The incidence and prevalence of hypertension are rising even among young people in both urban as well as rural communities. Although various conventional therapeutic moieties are available for the management of hypertension, they have serious flaws such as hepatic metabolism, reduced dose frequency, poor aqueous solubility, reduced bioavailability, and increased adverse effects, making the drug therapy ineffective. Therefore, it is required to design a novel drug delivery system having the capability to solve the constraints associated with conventional treatment of hypertension. Nanotechnology is a new way of using and manipulating the matter at the molecular level, whose functional organization is measured in nanometers. The applications of nanotechnology in the field of medicine provide an alternative and novel direction for the treatment of cardiovascular diseases and show excellent performance in the field of targeted drug therapy. Various nanotechnologies based drug delivery systems, such as solid lipid nanoparticles, nanosuspension, nanoemulsion, liposome, self-emulsifying systems, and polymeric nanoparticles, are available. Among them, nanoemulsion has provided a niche to supplement currently available therapeutic choices due to numerous benefits like stability, ease of preparation, enhanced drug absorption, reduced hepatic metabolism, increased dose frequency, enhanced bioavailability, and encapsulation of hydrophilic as well as hydrophobic drugs. This present review provides an in-depth idea about progression in treatment of hypertension, constraints for antihypertensive drug therapy, need of nanoemulsions to overcome these constraints, comparative analysis of nanoemulsions over other nanostructure drug delivery systems, pharmacodynamics studies of nanoemulsions for treatment of hypertension, recent patents for drug-loaded nanoemulsions meant for hypertension, and marketed formulations of nanoemulsions for hypertension.

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Enhanced bioavailability and antihypertensive activity of nisoldipine loaded nanoemulsion: optimization, cytotoxicity and uptake across Caco-2 cell line, pharmacokinetic and pharmacodynamic studies

Cited by 16 publications

References 39 publications

Microemulsion Delivery System Improves Cellular Uptake of Genipin and Its Protective Effect against Aβ1-42-Induced PC12 Cell Cytotoxicity

Microemulsion Delivery System Improves Cellular Uptake of Genipin and Its Protective Effect against Aβ1-42-Induced PC12 Cell Cytotoxicity

Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis

A Revolutionary Blueprint for Mitigation of Hypertension via Nanoemulsion

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