Essential oils: from extraction to encapsulation.

Protein-based nanocarriers as promising drug and gene delivery systems

Essential oils are complex blends of a variety of volatile molecules such as terpenoids, phenol-derived aromatic components, and aliphatic components having a strong interest in pharmaceutical, sanitary, cosmetic, agricultural, and food industries. Since the middle ages, essential oils have been widely used for bactericidal, virucidal, fungicidal, antiparasitical, insecticidal, and other medicinal properties such as analgesic, sedative, anti-inflammatory, spasmolytic, and locally anaesthetic remedies. In this review their nanoencapsulation in drug delivery systems has been proposed for their capability of decreasing volatility, improving the stability, water solubility, and efficacy of essential oil-based formulations, by maintenance of therapeutic efficacy. Two categories of nanocarriers can be proposed: polymeric nanoparticulate formulations, extensively studied with significant improvement of the essential oil antimicrobial activity, and lipid carriers, including liposomes, solid lipid nanoparticles, nanostructured lipid particles, and nano- and microemulsions. Furthermore, molecular complexes such as cyclodextrin inclusion complexes also represent a valid strategy to increase water solubility and stability and bioavailability and decrease volatility of essential oils.

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Essential Oils Loaded in Nanosystems: A Developing Strategy for a Successful Therapeutic Approach

Solid lipid nanoparticles and nanostructured lipid carriers: A review emphasizing on particle structure and drug release

Microemulsion utility in pharmaceuticals: Implications for multi-drug delivery.

The aim of the present study was to prepare solid lipid nanoparticles (SLNs) for the oral delivery of frankincense and myrrh essential oils (FMO). Aqueous dispersions of SLNs were successfully prepared by a high-pressure homogenization method using Compritol 888 ATO as the solid lipid and soybean lecithin and Tween 80 as the surfactants. The properties of the SLNs such as particle size, zeta potential (ZP), and drug encapsulation efficiency (EE) were investigated. The morphology of SLNs was observed by transmission electron microscopy (TEM). The crystallinity of the formulation was analyzed by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). In addition, drug evaporation release and antitumor activity were also studied. Round SLNs with a mean size of 113.3 ± 3.6 nm, a ZP of -16.8 ± 0.4 mV, and an EE of 80.60% ± 1.11% were obtained. DSC and XRD measurements revealed that less ordered structures were formed in the inner cores of the SLN particles. Evaporation loss of the active components in FMO could be reduced in the SLNs. Furthermore, the SLN formulation increased the antitumor efficacy of FMO in H22-bearing Kunming mice. Hence, the presented SLNs can be used as drug carriers for hydrophobic oil drugs extracted from traditional Chinese medicines.

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Preparation and characterization of solid lipid nanoparticles loaded with frankincense and myrrh oil

Bioadhesion and enhanced bioavailability by wheat germ agglutinin-grafted lipid nanoparticles for oral delivery of poorly water-soluble drug bufalin.

In the present study, nanostructured lipid carriers (NLCs) were prepared and optimized for the intravenous delivery of β-Elemene (β-E). Aqueous dispersions of NLCs were successfully prepared by high-pressure homogenization method using glycerol monostearate as the solid lipid and a mixture of Maisine 35-1 and Labrafil M1944 CS as the liquid lipid. The results revealed that the morphology of the NLCs was spheroidal. The particle size, zeta potential, and entrapment efficiency (EE) for the optimized formulation were observed as 138.9 nm, −20.2 mV, and 82.11%, respectively. X-ray diffraction analysis revealed the formation of less ordered structures in the inner core of the NLC particles. Moreover, the β-E-loaded NLCs were also less irritating and less toxic compared to Elemene injection. In addition, β-E-NLCs showed a significantly higher bioavailability and anti-tumor efficacy than Elemene injection. Taken together, our data indicate that the β-E-NLCs described in this study are well-suited for the intravenous delivery of β-E.

https://www.dovepress.com/getfile.php?fileID=16806

Formulation design, preparation, and in vitro and in vivo characterizations of β-Elemene-loaded nanostructured lipid carriers.

Objective: The purpose of this study was to improve skin permeation of evodiamine and rutaecarpine for transdermal delivery with microemulsion as vehicle and investigate real-time cutaneous absorption of the drugs via in vivo microdialysis. Methods: Pseudoternary phase diagrams were constructed to evaluate microemulsion regions with various surfactants and cosurfactants. Nine formulations of oil in water microemulsions were selected as vehicles for assessing skin permeation of evodiamine and rutaecarpine in ex vivo transdermal experiments. With a microdialysis hollow fiber membrane implanted in the skin beneath the site of topical drug administration, dialysis sampling was maintained for 10 hours and the samples were detected directly by high performance liquid chromatography. Real-time concentrations of the drugs in rat skin were investigated and compared with those of conventional formulations, such as ointment and tincture. Furthermore, the drugs were applied to various regions of the skin using microemulsion as vehicle. Results: In ex vivo transdermal experiments, cutaneous fluxes of evodiamine and rutaecarpine microemulsions were 2.55-fold to 11.36-fold and 1.17-fold to 6.33-fold higher, respectively, than those of aqueous suspensions. Different drug loadings, microemulsion water content, and transdermal enhancers markedly influenced the permeation of evodiamine and rutaecarpine. In microemulsion application with in vivo microdialysis, the maximum concentration of the drugs (evodiamine: 18.23 ± 1.54 ng/mL; rutaecarpine: 16.04 ± 0.69 ng/mL) were the highest, and the area under the curve 0–t of evodiamine and rutaecarpine was 1.52-fold and 2.27-fold higher than ointment and 3.06-fold and 4.23-fold higher than tincture, respectively. A greater amount of drugs penetrated through and was absorbed by rat abdominal skin than shoulder and chest, and a reservoir in the skin was found to supply drugs even after the microemulsion was withdrawn. Conclusion: Compared to conventional formulations, higher cutaneous fluxes of evodiamine and rutaecarpine were achieved with microemulsion. Based on this novel transdermal delivery, the transdermal route was effective for the administration of the two active alkaloids.

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Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion.

Preparation of a micro/nanotechnology based multi-unit drug delivery system for a Chinese medicine Niuhuang Xingxiao Wan and assessment of its antitumor efficacy.

Feng Shi

Papers

Preparation and characterization of solid lipid nanoparticles loaded with frankincense and myrrh oil

Bioadhesion and enhanced bioavailability by wheat germ agglutinin-grafted lipid nanoparticles for oral delivery of poorly water-soluble drug bufalin.

Formulation design, preparation, and in vitro and in vivo characterizations of β-Elemene-loaded nanostructured lipid carriers.

Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion.

Preparation of a micro/nanotechnology based multi-unit drug delivery system for a Chinese medicine Niuhuang Xingxiao Wan and assessment of its antitumor efficacy.