Nanocrystals for dermal penetration enhancement – Effect of concentration and underlying mechanisms using curcumin as model

Vidlářová, Lucie; Romero, Gregori B.; Hanuš, Jaroslav; Štěpánek, František; Müller, Rainer H.

doi:10.1016/j.ejpb.2016.05.004

Cited by 99 publications

(43 citation statements)

References 15 publications

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“…To reduce the size of large coarse particles, the top-down method utilizes highpressure homogenization or milling. [21] In the bottom-up approach, methods, such as nanoprecipitation are utilized to disperse NCs in aqueous solutions. [22] The nanoprecipitation method has several privileges, including low energy processes, simple instruments, decreased cost, and low temperature process that are compatible with thermosensitive drugs.…”

Section: Introductionmentioning

confidence: 99%

Fabrication of Carboxymethyl Chitosan Nanoparticles to Deliver Paclitaxel for Melanoma Treatment

et al. 2020

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In the present study, the effectiveness of paclitaxel nanocrystals (PTX NCs) encapsulated in carboxymethyl chitosan (CMCS) nanoparticles (CMCS−PTX NPs) as an anticancer drug is evaluated. The CMCS nanoparticles are produced via a cross‐junction microfluidic device where the PTX/CMCS concentration and flow rates in the device are optimized. The dynamic light scattering data show that the PTX NCs have a median diameter size of 230±90 nm, while the size of CMCS−PTX NPs is roughly 270±30 nm. The zeta‐potential result indicates less negative surface charge for the CMCS−PTX NPs as compared to the PTX NCs. Moreover, scanning electron microscopy micrographs, differential scanning calorimetry thermograms, and X‐ray diffraction patterns reveal that the physicochemical properties of the drug remain unaltered after perfusion through the microfluidic device. Cytotoxicity and cell endocytosis of PTX NCs and CMCS−PTX NPs are evaluated in vitro using G361 melanoma‐positive skin cells. The results reveal that the CMCS−PTX NPs increase the cellular uptake and cytotoxicity compared to the PTX NCs alone. In addition, the antitumor effect of CMCS−PTX NPs on B16 melanoma indicates the great potential of CMCS as a promising nano‐carrier for PTX NCs drug with potent inhibitory effect on the tumor growth.

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Section: Introductionmentioning

confidence: 99%

Fabrication of Carboxymethyl Chitosan Nanoparticles to Deliver Paclitaxel for Melanoma Treatment

et al. 2020

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“…Thus, nanocrystals offer several advantages and disadvantages. Among the advantages, there are: Possibility of administering a drug through different administration routes (oral, intravenous, intramuscular, pulmonary, ocular, dermal) [ 7 , 8 , 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 ]; Possibility of formulating a drug under different pharmaceutical dosage forms (tablets, capsules, suspensions, ointments, etc.) [ 17 , 25 , 26 , 27 , 28 , 29 ]; Higher solubility (thermodynamic or kinetic depending on the solid physical state of the drug) than conventional particles [ 8 , 17 , 22 , 23 , 30 , 31 , 32 ]; Faster dissolution rate than conventional particles [ 3 , 8 , 9 , 16 , 30 , 33 , 34 , 35 ]; Long circulating nanocrystals [ 36 , 37 <...>…”

Section: Introductionmentioning

confidence: 99%

“…Possibility of administering a drug through different administration routes (oral, intravenous, intramuscular, pulmonary, ocular, dermal) [ 7 , 8 , 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 ];…”

Section: Introductionmentioning

confidence: 99%

Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability

et al. 2018

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Many approaches have been developed over time to overcome the bioavailability limitations of poorly soluble drugs. With the advances in nanotechnology in recent decades, science and industry have been approaching this issue through the formulation of drugs as nanocrystals, which consist of “pure drugs and a minimum of surface active agents required for stabilization”. They are defined as “carrier-free submicron colloidal drug delivery systems with a mean particle size in the nanometer range, typically between 10–800 nm”. The primary importance of these nanoparticles was the reduction of particle size to nanoscale dimensions, with an increase in the particle surface area in contact with the dissolution medium, and thus in bioavailability. This approach has been proven successful, as demonstrated by the number of such drug products on the market. Nonetheless, despite the definition that indicates nanocrystals as a “carrier-free” system, surface active agents are necessary to prevent colloidal particles aggregation and thus improve stability. In addition, in more recent years, nanocrystal properties and technologies have attracted the interest of researchers as a means to obtain colloidal particles with modified biological properties, and thus their interest is now also addressed to modify the drug delivery and targeting. The present work provides an overview of the achievements in improving the bioavailability of poorly soluble drugs according to their administration route, describes the methods developed to overcome physicochemical and stability-related problems, and in particular reviews different stabilizers and surface agents that are able to modify the drug delivery and targeting.

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“…155 More examples of herbal loaded NE are presented in Table 1. [156][157][158][159][160][161][162][163] Phytosome or Herbosome Water-soluble phytochemicals such as flavonoids and polyphenols are poorly absorbed in the body due to their large molecular size which did not allow them to be absorbed by passive diffusion, as well as their poor lipid solubility makes a serious limiting to their pass across the lipid-rich biological membranes, subsequent poor bioavailability. 164 Phytosome is a patented formula developed to incorporate medicinal plant active ingredients and water-soluble phytochemicals into phospholipids to create lipid-compatible molecular complexes in order to immensely modify their absorption and bioavailability.…”

Section: Micellementioning

confidence: 99%

<p>Novel Drug Delivery Systems for Loading of Natural Plant Extracts and Their Biomedical Applications</p>

Rahman

Othman

Hammadi

et al. 2020

IJN

156

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Many types of research have distinctly addressed the efficacy of natural plant metabolites used for human consumption both in cell culture and preclinical animal model systems. However, these in vitro and in vivo effects have not been able to be translated for clinical use because of several factors such as inefficient systemic delivery and bioavailability of promising agents that significantly contribute to this disconnection. Over the past decades, extraordinary advances have been made successfully on the development of novel drug delivery systems for encapsulation of plant active metabolites including organic, inorganic and hybrid nanoparticles. The advanced formulas are confirmed to have extraordinary benefits over conventional and previously used systems in the manner of solubility, bioavailability, toxicity, pharmacological activity, stability, distribution, sustained delivery, and both physical and chemical degradation. The current review highlights the development of novel nanocarrier for plant active compounds, their method of preparation, type of active ingredients, and their biomedical applications.

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Nanocrystals for dermal penetration enhancement – Effect of concentration and underlying mechanisms using curcumin as model

Cited by 99 publications

References 15 publications

Fabrication of Carboxymethyl Chitosan Nanoparticles to Deliver Paclitaxel for Melanoma Treatment

Fabrication of Carboxymethyl Chitosan Nanoparticles to Deliver Paclitaxel for Melanoma Treatment

Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability

<p>Novel Drug Delivery Systems for Loading of Natural Plant Extracts and Their Biomedical Applications</p>

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