Design, formulation, in vitro, in vivo, and pharmacokinetic evaluation of nisoldipine-loaded self-nanoemulsifying drug delivery system

Balakumar, K; Rahman, Habibur; selvan, Natarajan Tamil; prasad, Ranganathan Hari; Rajkumar, M.; Selvakumar, M.; Vamshikrishna, K.; Marslin, Gregory; Vijayaraghavan, C.

doi:10.1007/s11051-014-2818-z

Cited by 28 publications

(19 citation statements)

References 35 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Other potential advantages of using SMEDDS to improve the oral bioavailability of poor water-soluble drugs are their promotion of transcellular and paracellular absorption, reduction of metabolism of CYP/CYP450 by gastrointestinal enzymes, and enhancement of lymphatic transport, all of which can protect the drug from first-pass metabolism. [18][19][20][21] In this study, we developed and optimized a TCG-loaded SMEDDS (TCG-SM) formulation by design of experiments using Scheffé's mixture design based on a small number of trials and response surface methodology. We also characterized the optimized TCG-SM, evaluated its in vitro dissolution, performed cellular studies, and compared its antiplatelet activity and pharmacokinetics with those of a raw TCG suspension.…”

Section: Introductionmentioning

confidence: 99%

<p>Strategic approach to developing a self-microemulsifying drug delivery system to enhance antiplatelet activity and bioavailability of ticagrelor</p>

Na¹,

Byeon²,

Wang³

et al. 2019

IJN

View full text Add to dashboard Cite

co. ltd., sejong, republic of Korea; 3 sama Pharmaceutical co. ltd., suwon, republic of Korea Background: Ticagrelor (TCG) is used to inhibit platelet aggregation in patients with acute coronary syndrome, but its poor solubility and low bioavailability limit its in vivo efficacy. The purpose of this study was to manufacture an optimized TCG-loaded self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability and antiplatelet activity of TCG. Materials and methods: Solubility and emulsification tests were conducted to determine the most suitable oils, surfactants, and cosurfactants. Scheffé's mixture design was applied to optimize the percentage of each component applied in the SMEDDS formulation to achieve optimal physical characteristics, ie, high solubility of TCG in SMEDDS, small droplet size, low precipitation, and high transmittance. Results: The optimized TCG-loaded SMEDDS (TCG-SM) formulation composed of 10.0% Capmul MCM (oil), 53.8% Cremophor EL (surfactant), and 36.2% Transcutol P (cosurfactant) significantly improving the dissolution of TCG in various media compared with TCG in Brilinta ® (commercial product). TCG-SM exhibited higher cellular uptake and permeability in Caco-2 cells than raw TCG suspension. In pharmacokinetic studies in rats, TCG-SM exhibited higher oral bioavailability with 5.7 and 6.4 times higher area under the concentration-time curve and maximum plasma concentration, respectively, than a raw TCG suspension. Antiplatelet activity studies exhibited that the TCG-SM formulation showed significantly improved inhibition of platelet aggregation compared with raw TCG at the same dose of TCG. And, a 10 mg/kg dose of raw TCG suspension and a 5 mg/kg dose of TCG-SM had a similar area under the inhibitory curve (907.0%±408.8% and 907.8%±200.5%⋅hours, respectively) for antiplatelet activity. Conclusion: These results suggest that the developed TCG-SM could be successfully used as an efficient method to achieve the enhanced antiplatelet activity and bioavailability of TCG.

show abstract

Section: Introductionmentioning

confidence: 99%

<p>Strategic approach to developing a self-microemulsifying drug delivery system to enhance antiplatelet activity and bioavailability of ticagrelor</p>

Na¹,

Byeon²,

Wang³

et al. 2019

IJN

View full text Add to dashboard Cite

show abstract

“…[1][2][3][4][5] Microemulsions have also been identified as potential delivery systems for bioactives in foods, pharmaceutical and cosmetic formulations. 6 There are several types of nanostructures, and microemulsions (MEs) are one of them, that can be used as carriers for lipophilic bioactive compounds, drugs or nutrients.…”

Section: Introductionmentioning

confidence: 99%

Microemulsion of Brazil nut oil as a natural product to improve superoxide release in human phagocytes

et al. 2017

View full text Add to dashboard Cite

The aim of this study was to develop and characterize a Brazil nut oil microemulsion system and determine the effect of this microemulsion on the superoxide release in human phagocytes. The microemulsion was formulated using distilled water, Brazil nut as the oily phase, Sorbitan monooleate, Polysorbate 80, and butan-1-ol. Hydrophile-lipophile balance of Brazil nut oil was determined, pseudoternary diagrams were prepared, and microemulsion diagram regions were preselected. Preliminary and accelerated stability tests, rheological characterization and dynamic light scattering were performed. The immunomodulatory effect of the microemulsion on the interactions with leukocytes was determined by superoxide release. The developed formulations were classified as oil-in-water, showed a Newtonian profile, with linear viscosity and droplet sizes of 46.9; 66.5 and 34.3 nm. When we assessed the interaction of the microemulsion of Brazil nut oil with phagocytes, we observed an increase in superoxide release. Our findings indicate that the developed formulation improved the immunomodulatory activity of the Brazil nut oil, proving to be a natural product option for future applications, in particular for infectious diseases.

show abstract

“…33 However, the oral bioavailability of the drug is only about 5% of the overall administered dose, due to very low aqueous solubility and high presystemic metabolism. 34 In an attempt to improve the solubility and oral bioavailability of the compound, 100 nanosize compositions with varying concentrations of different oils (25%-70% w:w), surfactants (30%-75% w:w), and cosurfactants (0-25% w:w) were prepared. From the initial panel, two nanocarrier formulations were selected as potential candidates for effective drug delivery based on solubility, stability over time, droplet size (one of the most important characteristics for stability evaluation and in vivo absorption), particle-size distribution, and negative ζ-potential.…”

Section: Diseases Of the Circulatory Systemmentioning

confidence: 99%

“…The study concluded that the optimized ACP19 formulation enhances the solubility and bioavailability of nisoldipine. 34 Olmesartan medoxomil is a potent angiotensin II receptor antagonist clinically used for the treatment and management of hypertension. 35 However, the drug exhibits low and inconsistent oral bioavailability in humans, primarily due to its high lipophilicity.…”

Section: Diseases Of the Circulatory Systemmentioning

confidence: 99%

Nanodelivery systems and stabilized solid-drug nanoparticles for orally administered medicine: current landscape

Kermanizadeh¹,

Powell²,

Stone³

2018

IJN

View full text Add to dashboard Cite

The use of nanoparticles as a means of targeted delivery of therapeutics and imaging agents could greatly enhance the transport of biologically active contents to specific target tissues, while avoiding or reducing potentially undesired side effects. Generally speaking, the oral route of administration is associated with good patient compliance, as it is convenient, economical, noninvasive, and does not require special training. Here, we review the progress of the utilization of nanodelivery-system carriers or stabilized solid-drug nanoparticles following oral administration, with particular attention on toxicological data. Mechanisms of cytotoxicity are discussed and the problem of extrapolating knowledge to human scenarios highlighted. Additionally, issues associated with administration of drugs via the oral route are underlined, while strategies utilized to overcome these are highlighted. This review aims to offer a balanced overview of strategies currently being used in the application of nanosize constructs for oral medical applications.

show abstract

Design, formulation, in vitro, in vivo, and pharmacokinetic evaluation of nisoldipine-loaded self-nanoemulsifying drug delivery system

Cited by 28 publications

References 35 publications

<p>Strategic approach to developing a self-microemulsifying drug delivery system to enhance antiplatelet activity and bioavailability of ticagrelor</p>

<p>Strategic approach to developing a self-microemulsifying drug delivery system to enhance antiplatelet activity and bioavailability of ticagrelor</p>

Microemulsion of Brazil nut oil as a natural product to improve superoxide release in human phagocytes

Nanodelivery systems and stabilized solid-drug nanoparticles for orally administered medicine: current landscape

Contact Info

Product

Resources

About