Aim: We aimed to develop nanoemulsions containing phosphodiesterase 4 inhibitor rolipram with different droplet sizes, to evaluate the anti-inflammatory effect against activated neutrophils and a related lung injury. Materials & methods: We prepared nanoemulsions of three different sizes, 68, 133 and 188 nm. Results: The nanoemulsion inhibited the superoxide anion but not elastase release in primary human neutrophils. The large-sized nanoemulsions were mostly internalized by neutrophils, resulting in the reduction of intracellular Ca2+ half-life. The peripheral organ distribution of near-infrared dye-tagged nanoemulsions increased, following the decrease in droplet diameter. Rolipram entrapment into intravenous nanoemulsions ameliorated pulmonary inflammation. The smallest droplet size showed improvement, compared with the largest size. Conclusion: We established a foundation for the development of nanoemulsions against inflamed lung disease.
- MeSH
- Anti-Inflammatory Agents * pharmacology MeSH
- Emulsions MeSH
- Humans MeSH
- Nanomedicine MeSH
- Neutrophils drug effects MeSH
- Inflammation * drug therapy MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
To provide the bilateral advantages of emulsions and hydrogels, a facile approach was used to fabricate nanoemulsions filled hydrogel beads through combining the method of self-emulsification and sodium alginate (SA) ionic gelation. The encapsulation and release behavior of curcumin (Cur) were further investigated. The results indicated that Cur packaged nanoemulsions were with the size of 24.26 ± 0.22 nm. The nanoemulsions filled SA hydrogel beads were spherical shell with the diameter of 0.46 ± 0.02 mm. For Cur, the EE and LC of emulsion filled SA hydrogel beads were 99.15 ± 0.85% and 7.25 ± 3.16 mg/g respectively. The release behavior could be regulated by external pH condition. The release behavior at pH 9.0 displayed a higher release rate than that at pH 7.0. Cur released behavior well followed the Hixcon-Crowell model which indicated that Cur was released in a diffusion-controlled model. Comparatively investigation of microstructure using field emission scanning electron microscope (FE-SEM) further investigates the corrosion behavior of SA gel beads during Cur release. The worth-while endeavor provided a practical combined technique of emulsions and ionic gelation to fabricate hybrid hydrogel beads that have potential in delivery system for hydrophobic composition.
- MeSH
- Alginates chemistry MeSH
- Emulsions MeSH
- Hydrophobic and Hydrophilic Interactions MeSH
- Hydrogels chemistry MeSH
- Kinetics MeSH
- Curcumin chemistry MeSH
- Microspheres * MeSH
- Nanostructures chemistry MeSH
- Drug Carriers chemistry MeSH
- Capsules MeSH
- Drug Liberation * MeSH
- Publication type
- Journal Article MeSH
Cannabidiol (CBD) is the non-psychoactive component of the plant Cannabis sativa (L.) that has great anti-inflammatory benefits and wound healing effects. However, its high lipophilicity, chemical instability, and extensive metabolism impair its bioavailability and clinical use. Here, we report on the preparation of a human cornea substitute in vitro and validate this substitute for the evaluation of drug penetration. CBD nanoemulsion was developed and evaluated for stability and biological activity. The physicochemical properties of CBD nanoemulsion were maintained during storage for 90 days under room conditions. In the scratch assay, nanoformulation showed significantly ameliorated wound closure rates compared to the control and pure CBD. Due to the lower cytotoxicity of nanoformulated CBD, a higher anti-inflammatory activity was demonstrated. Neither nanoemulsion nor pure CBD can penetrate the cornea after the four-hour apical treatment. For nanoemulsion, 94 % of the initial amount of CBD remained in the apical compartment while only 54 % of the original amount of pure CBD was detected in the apical medium, and 7 % in the cornea, the rest was most likely metabolized. In summary, the nanoemulsion developed in this study enhanced the stability and biological activity of CBD.
- MeSH
- Anti-Inflammatory Agents pharmacology MeSH
- Biological Availability MeSH
- Wound Healing MeSH
- Cannabidiol * chemistry MeSH
- Humans MeSH
- Cornea MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
Dyslipidemias are lipid metabolism alterations that cause increased levels of serum lipoprotein, cholesterol, and triglycerides. These alterations are associated with a higher incidence of cardiovascular diseases and are a risk factor for atherosclerosis development. This study aimed to evaluate the effect of Rosmarinus officinalis essential oil (EORO, 100 mg/kg) and its nanoemulsion (NEORO, 500 µg/kg) on Triton and coconut saturated-fat-induced (CSF) dyslipidemias using Wistar rats. The phytochemical evaluation of EORO performed by gas chromatography-mass spectroscopy (GC-MS) revealed 1,8-cineole (33.70%), camphor (27.68%), limonene (21.99%), and α-pinene (8.13%) as its major compounds. Triton-induced dyslipidemia significantly increased total cholesterol, LDL, and triglycerides levels. On the other hand, the groups treated with EORO and NEORO had significantly reduced total cholesterol, LDL, and triglycerides compared to the group treated only with Triton. Similar results were observed on the positive control treated with simvastatin. Dyslipidemia induced with coconut saturated-fat (CSF) caused abdominal fat gain, hypercholesterolemia, hypertriglyceridemia, increased LDL levels, and atherogenesis in the aorta. In contrast, the groups treated with EORO, NEORO, and simvastatin had significantly reduced hypercholesterolemia and hypertriglyceridemia, reduced abdominal fat gain, and absence of atherogenesis in the vascular endothelium. Overall, in the Triton-induced dyslipidemia model, EORO treatment had superior values than NEORO's (and simvastatin), although the differences were not too high, while in the CSF model, the values were mixed. In this manner, our results show an anti-dyslipidemic and anti-atherogenic activity effect by EORO and NEORO.
- Keywords
- nanoemulze,
- MeSH
- Aorta, Thoracic diagnostic imaging pathology MeSH
- Atherosclerosis drug therapy complications MeSH
- Chromatography statistics & numerical data MeSH
- Dyslipidemias * drug therapy complications MeSH
- Microscopy, Electron, Scanning MeSH
- Models, Animal MeSH
- Nanostructures statistics & numerical data therapeutic use MeSH
- Oils, Volatile * analysis administration & dosage chemistry MeSH
- Rats, Wistar MeSH
- Rosmarinus MeSH
- Simvastatin therapeutic use MeSH
- Fats adverse effects MeSH
- Treatment Outcome MeSH
- Publication type
- Clinical Study MeSH
- Research Support, Non-U.S. Gov't MeSH
This review describes a new trend in the formulation of dosage forms containing poorly water-soluble drugs lipophilic solutions, dispersions, liposomes and nanoparticles dealing also with their composition and manufacture. The dispersions are further divided into nonemulsifying, self-emulsifying, self-microemulsifying and self-nanoemulsifying drug delivery systems. The cited systems are able to form micro- and nanoemulsions in contact with gastric juices. Formulations containing lipophilic nanoparticles as well as micro- and nanoemulsions are easily absorbed. A system classifying lipid formulations according to the drug composition is also described. The system enables the taxonomy of lipophilic drugs to be made; it also tries to describe their further metabolic ways in the organism.
Although many pharmaceuticals have therapeutic potentials for central nervous system (CNS) diseases, few of these agents have been effectively administered. It is due to the fact that the blood-brain barrier (BBB) and the blood-cerebrospinal fluid barrier (BCSF) restrict them from crossing the brain to exert biological activity. This article reviews the current approaches aiming to improve penetration across these barriers for effective drug delivery to the CNS. These issues are summarized into direct systemic delivery and invasive delivery, including the BBB disruption and convection enhanced delivery. Furthermore, novel drug delivery systems used at the nanoscale, including polymeric nanoparticles, liposomes, nanoemulsions, dendrimers, and micelles are discussed. These nanocarriers could contribute to a breakthrough in the treatment of many different CNS diseases. However, further broadened studies are needed to assess the biocompatibility and safety of these medical devices.
- MeSH
- Central Nervous System * MeSH
- Drug Delivery Systems * MeSH
- Publication type
- Journal Article MeSH
- Review MeSH
The use of natural compounds is becoming increasingly popular among patients, and there is a renewed interest among scientists in nature-based bioactive agents. Traditionally, herbal drugs can be taken directly in the form of teas/decoctions/infusions or as standardized extracts. However, the disadvantages of natural compounds, especially essential oils, are their instability, limited bioavailability, volatility, and often irritant/allergenic potential. However, these active substances can be stabilized by encapsulation and administered in the form of nanoparticles. This brief overview summarizes the latest results of the application of nanoemulsions, liposomes, solid lipid nanoparticles, and nanostructured lipid carriers used as drug delivery systems of herbal essential oils or used directly for their individual secondary metabolites applicable in cancer therapy. Although the discussed bioactive agents are not typical compounds used as anticancer agents, after inclusion into the aforesaid formulations improving their stability and bioavailability and/or therapeutic profile, they indicated anti-tumor activity and became interesting agents with cancer treatment potential. In addition, co-encapsulation of essential oils with synthetic anticancer drugs into nanoformulations with the aim to achieve synergistic effect in chemotherapy is discussed.
- Publication type
- Journal Article MeSH
- Review MeSH
Imiquimod (IMQ) is an immunostimulating agent used in the treatment of basal cell carcinoma and actinic keratosis. Due to its low solubility and poor skin bioavailability, the dermal formulation of IMQ remains challenging. In analogy to tyre compounds used in Formula 1 racing, we compare four types of nanosystems belonging to three groups: (i) "hard" nanoparticles in the form of IMQ nanocrystals, (ii) "intermediate" nanoparticles in the form of liposomes and lipid nanocapsules, and (iii) "soft" nanoparticles in the form of a nanoemulsion based on oleic acid. The nanoemulsion and nanocrystals were able to incorporate the highest amount of IMQ (at least 2 wt%) compared to liposomes (0.03 wt%) and lipid nanocapsules (0.08 wt%). Regarding size, liposomes, and lipid nanocapsules were rather small (around 40 nm) whereas nanocrystals and nanoemulsion were larger (around 200 nm). All developed nanoformulations showed high efficiency to deliver IMQ into the skin tissue without undesirable subsequent permeation through the skin to acceptor. Especially, the 2 wt% IMQ nanoemulsion accumulated 129 μg/g IMQ in the skin, compared to 34 μg/g of a 5 wt% commercial cream. The effects of the respective nanoparticulate systems were discussed with respect to their possible diffusion kinetics (Brownian motion vs. settling) in the aqueous phase.
- MeSH
- Imiquimod chemistry MeSH
- Skin metabolism MeSH
- Lipids pharmacology MeSH
- Liposomes * pharmacology MeSH
- Nanocapsules * MeSH
- Publication type
- Journal Article MeSH
Every year many drug molecules discovered to be effective in treatment of many diseases, however not all of these drugs succeed in reaching the market. One of the main reasons for such failure is the lipophilicity or low water solubility of these chemicals which results in poor bioavailability. Nanoemulsion has the ability to deliver these drugs in an efficient way. Nanoemulsion, which is usually o/w emulsion can incorporate this lipophilic drug into nanolipoidal droplets. However, the difficulty in applying liquid dosage form can be overcome by using nanoemulgel system. Nanoemulgel considered as a suitable way to deliver lipophilic drugs through topical route. This review tries to highlight the importance of nanoemulgel as a drug delivery system. The components of the systems have been explored and the methods of preparations including high energy methods and low energy methods have been discussed. Different methods were used in characterization of such delivery system; all of these methods and techniques were reviewed briefly. Finally, the recent researches about different applications of emulgel in local delivery or systemic delivery has been discussed. To conclude, the nanoemulgel applications in drug delivery is very promising and many products will find their way to the markets soon.
This study investigates the interaction of two approved and one newly developed latanoprost formulation with in vitro and in silico models of the tear film and tear film lipid layer (TFLL). Latanoprost, a prostaglandin analogue used for intraocular elevated pressure treatment, is topically delivered by nanocarriers within aqueous solutions or emulsions. The study focuses on the impact of these carriers on drug interactions with the tear film and their effect on the TFLL. Three different types of latanoprost carriers, micellar, nanoemulsion, and polymer-based, were compared, and each revealed distinct interaction patterns with the TFLL. Surface pressure kinetics demonstrated a rapid increase for the benzalkonium chloride formulation and a slow rise for the preservative-free variants. Visualization of the acellular in vitro TFLL model revealed different patterns of incorporation for each formulation, indicating unique interaction mechanisms. Molecular dynamics simulations further revealed different mechanisms of drug release in the TFLL between micellar and nanoemulsion formulations. In-depth examination highlighted the role of triglyceride molecules in replenishing the nonpolar layer of the TFLL, which suggests potential improvements in ocular surface compatibility by adjusting the quality and concentration of the oily phase. These findings suggest the potential for optimizing latanoprost formulations by tuning the oily phase-to-surfactant ratio and selecting suitable surfactants.
- MeSH
- Antihypertensive Agents therapeutic use MeSH
- Glaucoma * drug therapy MeSH
- Latanoprost therapeutic use MeSH
- Humans MeSH
- Intraocular Pressure MeSH
- Eye * MeSH
- Drug Delivery Systems MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
