Topotecan-loaded lipid nanoparticles as a viable tool for the topical treatment of skin cancers

Venâncio, João Hélio; Andrade, Lígia Marquez; Esteves, Najla; Brito, Lara Barroso; Valadares, Marize Campos; Oliveira, Gisele Augusto Rodrigues de; Lima, Eliana Martins; Marreto, Ricardo Neves; Gratieri, Taís; Taveira, Stephânia Fleury

doi:10.1111/jphp.12772

Cited by 22 publications

(7 citation statements)

References 28 publications

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“…A first way to control the release profile of a drug from a cellulose-based material is to design the complete drug delivery system based on surface charge interactions. Pure hydrogels of cellulosics were used to entrap lipid nanoparticles loaded with 5-fluorouracil [56] and topotecan [53] (two hydrophilic chemotherapeutic agents active against carcinoma), avanafil [55] (a hydrophobic molecule active in erectile dysfunction) and nano-emulsified copaiba oil [54] (anti-inflammatory essential oil).…”

Section: Hydrogels As Lipid Nanoparticle Scaffoldsmentioning

confidence: 99%

“…The study also showed that the anti-inflammatory effect of the complete system remained successfully equivalent to that of ketoprofen (a well-known non-steroidal anti-inflammatory drug). Venancio and collaborators [53] also pointed out that the neutral charge of HEC films encapsulating topotecan-loaded LNP allowed more of the lipid nanoparticles to be retained in the stratum corneum and in the deeper layers of the skin compared to LNP-loaded chitosan films. Because of its neutral charge, HEC polymer was then proven to have a wide range of application as LNP host.…”

Section: Hydrogels As Lipid Nanoparticle Scaffoldsmentioning

confidence: 99%

“…Among the different causes, the interactions between the protonated amine group of the chitosan network and the surface charges of LNE may trigger the aggregation of small droplets, explaining the increase in PDI values [54]. In addition, the strong electrostatic interactions between chitosan polar groups and the LNE surface charge prevent most of LNE from crossing the first skin barrier [53], explaining why less LNE remains on the stratum corneum after material application compared to the cellulosic-based LNE-hydrogel formulation [54]. However, LNE have been found in deeper layers of the skin when LNE-loaded chitosan hydrogels were used in comparison to cellulosic-based hydrogels.…”

Section: Hydrogels As Lipid Nanoparticle Scaffoldsmentioning

confidence: 99%

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Lipid Nanoparticles and Their Hydrogel Composites for Drug Delivery: A Review

2018

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Several drug delivery systems already exist for the encapsulation and subsequent release of lipophilic drugs that are well described in the scientific literature. Among these, lipid nanoparticles (LNP) have specifically come up for dermal, transdermal, mucosal, intramuscular and ocular drug administration routes in the last twenty years. However, for some of them (especially dermal, transdermal, mucosal), the LNP aqueous dispersions display unsuitable rheological properties. They therefore need to be processed as semi-solid formulations such as LNP-hydrogel composites to turn into versatile drug delivery systems able to provide precise spatial and temporal control of active ingredient release. In the present review, recent developments in the formulation of lipid nanoparticle-hydrogel composites are highlighted, including examples of successful encapsulation and release of lipophilic drugs through the skin, the eyes and by intramuscular injections. In relation to lipid nanoparticles, a specific emphasis has been put on the LNP key properties and how they influence their inclusion in the hydrogel. Polymer matrices include synthetic polymers such as poly(acrylic acid)-based materials, environment responsive (especially thermo-sensitive) polymers, and innovative polysaccharide-based hydrogels. The composite materials constitute smart, tunable drug delivery systems with a wide range of features, suitable for dermal, transdermal, and intramuscular controlled drug release.

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Section: Hydrogels As Lipid Nanoparticle Scaffoldsmentioning

confidence: 99%

Section: Hydrogels As Lipid Nanoparticle Scaffoldsmentioning

confidence: 99%

Section: Hydrogels As Lipid Nanoparticle Scaffoldsmentioning

confidence: 99%

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Lipid Nanoparticles and Their Hydrogel Composites for Drug Delivery: A Review

2018

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“…Various nanoparticle-mediated drug delivery systems are recently being investigated to check the chemical stability and improve the release profile of the antitumour drugs like TPT [ 1 , 3 ]. These drug delivery systems include lipid-based nanoparticles [ 4 ], mesoporous silica nanoparticles [ 5 ], solid lipid nanoparticles (SLNs) [ 6 ], and liposomes [ 7 ]. However, most of these studies did not report the complete profile of TPT including its antitumour capability, therapeutic efficacy, and safety profile, most particularly after rectal administration.…”

Section: Introductionmentioning

confidence: 99%

Development, Characterization, and Evaluation of SLN-Loaded Thermoresponsive Hydrogel System of Topotecan as Biological Macromolecule for Colorectal Delivery

Xing

Mustapha

Ali

et al. 2021

BioMed Research International

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Background. Chemotherapeutic drugs cause severe toxicities if administered unprotected, without proper targeting, and controlled release. In this study, we developed topotecan- (TPT-) loaded solid lipid nanoparticles (SLNs) for their chemotherapeutic effect against colorectal cancer. The TPT-SLNs were further incorporated into a thermoresponsive hydrogel system (TRHS) (TPT-SLNs-TRHS) to ensure control release and reduce toxicity of the drug. Microemulsion technique and cold method were, respectively, used to develop TPT-SLNs and TPT-SLNs-TRHS. Particle size, polydispersive index (PDI), and incorporation efficiency (IE) of the TPT-SLNs were determined. Similarly, gelation time, gel strength, and bioadhesive force studies of the TPT-SLNs-TRHS were performed. Additionally, in vitro release and pharmacokinetic and antitumour evaluations of the formulation were done. Results. TPT-SLNs have uniformly distributed particles with mean size in nanorange (174 nm) and IE of ~90%. TPT-SLNs-TRHS demonstrated suitable gelation properties upon administration into the rat’s rectum. Moreover, drug release was exhibited in a control manner over an extended period of time for the incorporated TPT. Pharmacokinetic studies showed enhanced bioavailability of the TPT with improved plasma concentration and AUC. Further, it showed significantly enhanced antitumour effect in tumour-bearing mice as compared to the test formulations. Conclusion. It can be concluded that SLNs incorporated in TRHS could be a potential source of the antitumour drug delivery with better control of the drug release and no toxicity.

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“…The major limitation of this drug is that TPT is unstable in physiological conditions and undergoes a pH-dependent rapid and reversible hydrolysis from a closed lactone ring to the inactive carboxylated open-ring form, which causes the loss of the antitumor activity of the drug [4]. To protect TPT from hydrolysis, the encapsulation into different types of nanoparticles such as liposomes, lipid nanoparticles, and mesoporous silica has been presented [5,6,7,8].…”

Section: Introductionmentioning

confidence: 99%

Rapid Microfluidic Preparation of Niosomes for Targeted Drug Delivery

Şeleci

Maurer

Stahl

et al. 2019

IJMS

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Niosomes are non-ionic surfactant-based vesicles with high promise for drug delivery applications. They can be rapidly prepared via microfluidics, allowing their reproducible production without the need of a subsequent size reduction step, by controlled mixing of two miscible phases of an organic (lipids dissolved in alcohol) and an aqueous solution in a microchannel. The control of niosome properties and the implementation of more complex functions, however, thus far are largely unknown for this method. Here we investigate microfluidics-based manufacturing of topotecan (TPT)-loaded polyethylene glycolated niosomes (PEGNIO). The flow rate ratio of the organic and aqueous phases was varied and optimized. Furthermore, the surface of TPT-loaded PEGNIO was modified with a tumor homing and penetrating peptide (tLyp-1). The designed nanoparticular drug delivery system composed of PEGNIO-TPT-tLyp-1 was fabricated for the first time via microfluidics in this study. The physicochemical properties were determined through dynamic light scattering (DLS) and zeta potential analysis. In vitro studies of the obtained formulations were performed on human glioblastoma (U87) cells. The results clearly indicated that tLyp-1-functionalized TPT-loaded niosomes could significantly improve anti-glioma treatment.

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Topotecan-loaded lipid nanoparticles as a viable tool for the topical treatment of skin cancers

Abstract: TPT-NLC-HEC may be a valuable tool for the topical treatment of skin cancers.

Cited by 22 publications

References 28 publications

Lipid Nanoparticles and Their Hydrogel Composites for Drug Delivery: A Review

Lipid Nanoparticles and Their Hydrogel Composites for Drug Delivery: A Review

Development, Characterization, and Evaluation of SLN-Loaded Thermoresponsive Hydrogel System of Topotecan as Biological Macromolecule for Colorectal Delivery

Rapid Microfluidic Preparation of Niosomes for Targeted Drug Delivery

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