Improved tacrolimus skin permeation by co-encapsulation with clobetasol in lipid nanoparticles: Study of drug effects in lipid matrix by electron paramagnetic resonance

Andrade, Lígia Marquez; Silva, Luís Antônio Dantas; Krawczyk-Santos, Anna Paula; Amorim, Isabella Cristina de S.M.; Rocha, Priscila Bianca Rodrigues da; Lima, Eliana Martins; Anjos, Jorge Luiz Vieira dos; Alonso, Antônio; Marreto, Ricardo Neves; Taveira, Stephânia Fleury

doi:10.1016/j.ejpb.2017.06.014

Cited by 27 publications

(12 citation statements)

References 39 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Both the stable cavitation intensity and inertial cavitation dose of DOX-MBs (500 µg) were lower than those of pure-lipid MBs. A previous study observed that adding drugs (tacrolimus, clobetasol) into lipid carriers reduced the lipid fluidity of a lipid matrix [42]. Considering these findings in combination with our microscopic observations, we concluded that a uniform distribution of DOX within the lipid shell would increase the shell stiffness of MBs by reducing lipid fluidity, thereby reducing the oscillation of MBs.…”

Section: Discussionsupporting

confidence: 82%

The Impact of Surface Drug Distribution on the Acoustic Behavior of DOX-Loaded Microbubbles

2021

View full text Add to dashboard Cite

Previous studies have reported substantial improvement of microbubble (MB)-mediated drug delivery with ultrasound when drugs are loaded onto the MB shell compared with a physical mixture. However, drug loading may affect shell properties that determine the acoustic responsiveness of MBs, producing unpredictable outcomes. The aim of this study is to reveal how the surface loaded drug (doxorubicin, DOX) affects the acoustic properties of MBs. A suitable formulation of MBs for DOX loading was first identified by regulating the proportion of two lipid materials (1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) and 1,2-distearoyl-sn-glycero-3-phospho-rac-glycerol sodium salt (DSPG)) with distinct electrostatic properties. We found that the DOX loading capacity of MBs was determined by the proportion of DSPG, since there was an electrostatic interaction with DOX. The DOX payload reduced the lipid fluidity of MBs, although this effect was dependent on the spatial uniformity of DOX on the MB shell surface. Loading DOX onto MBs enhanced acoustic stability 1.5-fold, decreased the resonance frequency from 12–14 MHz to 5–7 MHz, and reduced stable cavitation dose by 1.5-fold, but did not affect the stable cavitation threshold (300 kPa). Our study demonstrated that the DOX reduces lipid fluidity and decreases the elasticity of the MB shell, thereby influencing the acoustic properties of MBs.

show abstract

Section: Discussionsupporting

confidence: 82%

The Impact of Surface Drug Distribution on the Acoustic Behavior of DOX-Loaded Microbubbles

2021

View full text Add to dashboard Cite

show abstract

“…The SEM analysis was performed for morphological studies. The formulation coated with gold in nanostructure coating DSR1, and observed in HITACHI S-4160 SEM at an acceleration voltage of 20.0 kV and a magnification of 15000 X [13].…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Topical gel of Metformin solid lipid nanoparticles: A hopeful promise as a dermal delivery system

Rostamkalaei

Âkbari

Saeedi

et al. 2019

Colloids and Surfaces B: Biointerfaces

View full text Add to dashboard Cite

show abstract

“…Nevertheless, our previous research revealed that the retention of FK506 from the commercial ointment in the target skin site is deficient owing to the poor solubility, high molecular weight of drug, and the oil vehicle of ointment 9,10. Various nanocarriers including microemulsion (ME), ethosomes, nanoparticles, and lipid nanoparticles enhance drug penetration and target the skin,11–14 and ME offers greater properties than other nanocarriers with high drug-solubilizing capacity, long-term stability, and easy scale-up 15,16. Moreover, topical application of FK506 can evoke skin irritations of transient burning sensation at the beginning of therapy.…”

Section: Introductionmentioning

confidence: 99%

<p>Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects</p>

Wang¹,

Cao²,

Yu³

et al. 2019

IJN

View full text Add to dashboard Cite

Background: Topical application of tacrolimus (FK506) was effective in treating atopic dermatitis (AD); however, the therapeutic efficiency is hampered by its poor penetration into the skin and local side effects of transient irritation symptoms with a burning sensation, a feeling of warmth or heat. Menthol and camphor have been widely used in topical compound formulations for adjunctive pharmacotherapy for antipruritics and analgesics owing to their cool nature, and both present skin penetration enhancing effects. Moreover, they can form a liquid eutectic oil to solubilize hydrophobic drugs. Purpose: Taking advantages of menthol/camphor eutectic (MCE), this work aims to integrate FK506 into MCE to construct a microemulsion system, i.e., FK506 MCE ME, which simultaneously enhances the percutaneous delivery and treatment efficacy, while reduces the side effects of FK506. Methods: The formulation of FK506 MCE ME was optimized and characterized. Different formulations containing FK506 were topically administered to treat 1–chloro–2, 4–dinitrobenzene (DNCB)-induced murine AD. Results: MCE solubilized FK506. FK506 in MCE ME penetrated skin in vitro more than in the commercial ointment, and MCE predominantly exerted the enhancing effects in MCE ME. FK506 MCE ME or FK506 MCE ME gel had greater effects on clinical symptoms, histological analysis, and IgE than did commercial FK506. The anti-pruritic and down-regulation of substance P effects of MCE ME vehicle mitigated the side effects of FK506 application. Conclusion: MCE ME presented the excellent properties of simultaneously enhancing the percutaneous delivery and treatment efficacy, while reducing the side effects of FK506 for AD. Therefore, MCE ME is a promising nanoscale system for FK506 to effectively treating AD with low irritation and high medication adherence. Chemical compounds studied in this article: Tacrolimus (PubChem CID: 445643); menthol (PubChem CID: 1254); camphor (PubChem CID: 2537)

show abstract

Improved tacrolimus skin permeation by co-encapsulation with clobetasol in lipid nanoparticles: Study of drug effects in lipid matrix by electron paramagnetic resonance

Cited by 27 publications

References 39 publications

The Impact of Surface Drug Distribution on the Acoustic Behavior of DOX-Loaded Microbubbles

The Impact of Surface Drug Distribution on the Acoustic Behavior of DOX-Loaded Microbubbles

Topical gel of Metformin solid lipid nanoparticles: A hopeful promise as a dermal delivery system

<p>Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects</p>

Contact Info

Product

Resources

About