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Molecules (Basel, Switzerland) Aug 2023In the current study, clove oil nanoemulsion (CL-nanoemulsion) and emulsion (CL-emulsion) were prepared through an ecofriendly method. The prepared CL-nanoemulsion and...
In the current study, clove oil nanoemulsion (CL-nanoemulsion) and emulsion (CL-emulsion) were prepared through an ecofriendly method. The prepared CL-nanoemulsion and CL-emulsion were characterized using dynamic light scattering (DLS) and a transmission electron microscope (TEM), where results illustrated that CL-nanoemulsion droplets were approximately 32.67 nm in size and spherical in shape, while CL-nanoemulsion droplets were approximately 225.8 nm with a spherical shape. The antibacterial activity of CL-nanoemulsion and CL-emulsion was carried out using a microbroth dilution method. Results revealed that the preferred CL-nanoemulsion had minimal MIC values between 0.31 and 5 mg/mL. The antibiofilm efficacy of CL-nanoemulsion against significantly decreased the development of biofilm compared with CL-emulsion. Furthermore, results illustrated that CL-nanoemulsion showed antifungal activity significantly higher than CL-emulsion. Moreover, the prepared CL-nanoemulsion exhibited outstanding antifungal efficiency toward , , , , and where MICs were 12.5, 3.12, 0.78, 1.56, and 1.56 mg/mL, respectively. Additionally, the prepared CL-nanoemulsion was analyzed for its antineoplastic effects through a modified MTT assay for evaluating apoptotic and cytotoxic effects using HepG2 and MCF-7 cell lines. MCF-7 breast cancer cells showed the lowest IC values (3.4-fold) in CL-nanoemulsion relative to that of CL-emulsion. Thus, CL-nanoemulsion induces apoptosis in breast cancer cells by inducing caspase-8 and -9 activity and suppressing VEGFR-2. In conclusion, the prepared CL-nanoemulsion had antibacterial, antifungal, and antibiofilm as well as anticancer properties, which can be used in different biomedical applications after extensive studies in vivo.
Topics: Biofilms; Antineoplastic Agents; Oils, Volatile; Emulsions; Syzygium; Dynamic Light Scattering; Microscopy, Electron, Transmission; Hep G2 Cells; MCF-7 Cells; Humans; Apoptosis; Anti-Bacterial Agents; Antifungal Agents; Nanoparticle Drug Delivery System; Nanostructures; Staphylococcus aureus; Fungi
PubMed: 37570781
DOI: 10.3390/molecules28155812 -
Drug Delivery Dec 2022Self-emulsifying drug delivery systems (SEDDS) are a proven method for poorly soluble substances works by increasing the solubility and bioavailability. SEDDS and... (Review)
Review
Self-emulsifying drug delivery systems (SEDDS) are a proven method for poorly soluble substances works by increasing the solubility and bioavailability. SEDDS and isotropic mixtures, are composed of oils, surfactants, and occasionally cosolvents. The ability of these formulations and methods to produce microemulsions or fine oil-in-water (o/w) emulsions after moderate stirring and dilution by water phase along the GI tract might be a promising technique for lipophilic agents with dissolution rate-limited absorption. This review provides an outline of SEDDS's numerous advances and biopharmaceutical elements, types, manufacturing, characterization, limitations, and future prospects. The evaluation of SEDDS and its applications are also discussed, focusing on the advances of SEDDS's solid self-emulsifying delivery mechanism and dosage form. By integrating suitable polymer into the formulation, SEDDS may be studied for the creation of a formulation with sustained drug release. This technology's improvement might lead to a new application in the field of medicine delivery. SEDDS has been demonstrated to be quite efficient in increasing oral bioavailability of lipophilic products. SEDDS is one of the promising methods for controlling the characteristics of medications that are not great choices for oral delivery. It is also worth mentioning that SEDDS may be made in variety of solid dosage forms that are acceptable for both oral and parenteral administration.
Topics: Administration, Oral; Biological Availability; Drug Delivery Systems; Emulsions; Solubility; Water
PubMed: 35666090
DOI: 10.1080/10717544.2022.2083724 -
Biomedicine & Pharmacotherapy =... Mar 2022Atopic dermatitis (AD) is an inflammatory disorder centered around loss of epidermal barrier function, and T helper 2 (Th2) immune responses. The current understanding... (Review)
Review
Atopic dermatitis (AD) is an inflammatory disorder centered around loss of epidermal barrier function, and T helper 2 (Th2) immune responses. The current understanding of disease heterogeneity and complexity, limits the rational use of existing topical, systemic therapeutic agents, but paves way for development of advanced therapeutic agents. Additionally, advanced nanocarriers that deliver therapeutics to target cells, seem to offer a promising strategy, to overcome intrinsic limitations and challenges of conventional, and traditional drug delivery systems. Ever-evolving understanding of molecular target sites and complex pathophysiology, adverse effects of current therapeutic options, inefficient disease recapitulation by existing animal models are some of the challenges that we face. Also, despite limited success in market translatibility, nanocarriers have demonstrated excellent preclinical results and have been extensively studied for AD. Detailed research on behavior of nanocarriers in different patients and tailored therapy to account for phenotypic variability of the disease are the new research avenues that we look forward to.
Topics: Animals; Cytokines; Dermatitis, Atopic; Disease Models, Animal; Emulsions; Immune Tolerance; Inflammation Mediators; Liposomes; Microspheres; Nanoparticle Drug Delivery System; Skin; T-Lymphocytes, Regulatory
PubMed: 35030434
DOI: 10.1016/j.biopha.2022.112633 -
Molecular Pharmaceutics Sep 2023Delamanid (DLM) is a hydrophobic small molecule therapeutic used to treat drug-resistant tuberculosis (DR-TB). Due to its hydrophobicity and resulting poor aqueous...
Delamanid (DLM) is a hydrophobic small molecule therapeutic used to treat drug-resistant tuberculosis (DR-TB). Due to its hydrophobicity and resulting poor aqueous solubility, formulation strategies such as amorphous solid dispersions (ASDs) have been investigated to enhance its aqueous dissolution kinetics and thereby improve oral bioavailability. However, ASD formulations are susceptible to temperature- and humidity-induced phase separation and recrystallization under harsh storage conditions typically encountered in areas with high tuberculosis incidence. Nanoencapsulation represents an alternative formulation strategy to increase aqueous dissolution kinetics while remaining stable at elevated temperature and humidity. The stabilizer layer coating the nanoparticle drug core limits the formation of large drug domains by diffusion during storage, representing an advantage over ASDs. Initial attempts to form DLM-loaded nanoparticles via precipitation-driven self-assembly were unsuccessful, as the trifluoromethyl and nitro functional groups present on DLM were thought to interfere with surface stabilizer attachment. Therefore, in this work, we investigated the nanoencapsulation of DLM via emulsification, avoiding the formation of a solid drug core and instead keeping DLM dissolved in a dichloromethane dispersed phase during nanoparticle formation. Initial emulsion formulation screening by probe-tip ultrasonication revealed that a 1:1 mass ratio of lecithin and HPMC stabilizers formed 250 nm size-stable emulsion droplets with 40% DLM loading. Scale-up studies were performed to produce nearly identical droplet size distribution at larger scale using high-pressure homogenization, a continuous and industrially scalable technique. The resulting emulsions were spray-dried to form a dried powder, and dissolution studies showed dramatically enhanced dissolution kinetics compared to both as-received crystalline DLM and micronized crystalline DLM, owing to the increased specific surface area and partially amorphous character of the DLM-loaded nanoparticles. Solid-state NMR and dissolution studies showed good physical stability of the emulsion powders during accelerated stability testing (50 °C/75% RH, open vial).
Topics: Humans; Tuberculosis, Oral; Emulsions; Nanoparticles; Solubility; Excipients; Water; Particle Size
PubMed: 37578286
DOI: 10.1021/acs.molpharmaceut.3c00240 -
Chemical & Pharmaceutical Bulletin 2023Itraconazole, a commonly used antifungal drug in the clinic approved by U.S. Food and Drug Administration (FDA), has been gradually found to have anti-tumor,...
Itraconazole, a commonly used antifungal drug in the clinic approved by U.S. Food and Drug Administration (FDA), has been gradually found to have anti-tumor, angiogenesis inhibition and other pharmacological activities. However, its poor water solubility and potential toxicity limited its clinical application. In order to improve the water solubility and reduce the side effects caused by the high concentration of itraconazole, a novel preparation method of itraconazole sustained release microspheres was established in this study. Firstly, five kinds of polylactic acid-glycolic acid (PLGA) microspheres loaded with itraconazole were prepared by oil/water (O/W) emulsion solvent evaporation and then characterized by infrared spectroscopy. Then the particle size and morphology of the microspheres were observed by scanning electron microscope (SEM) and transmission electron microscope (TEM). After that, the particle size distribution, drug loading rate, entrapment efficiency, and drug release experiments were evaluated. Our results showed the microspheres prepared in this study had uniform particle size distribution and good integrity. Further study found that the average drug loading of the five kinds of microspheres prepared with PLGA 7505, PLGA 7510, PLGA 7520, PLGA 5020 and PLGA 0020 were 16.88, 17.72, 16.72, 16.57, and 16.64%, respectively, and the encapsulation rate all reached about 100%. More surprisingly, the release experimental results showed that the microspheres prepared with PLGA 7520 did not show sudden release, showing good sustained release performance and high drug release rate. To sum up, this study optimized the preparation method of sustained-release microspheres without sudden release, which provides a new solution for the delivery of itraconazole in the clinic.
Topics: Polylactic Acid-Polyglycolic Acid Copolymer; Polyglycolic Acid; Lactic Acid; Delayed-Action Preparations; Itraconazole; Microspheres; Emulsions; Solvents; Particle Size
PubMed: 37394601
DOI: 10.1248/cpb.c22-00747 -
Drug Delivery Dec 2021To evaluate the enhancement of temozolomide (TMZ) delivery in the rat brain using a triolein emulsion.
PURPOSE
To evaluate the enhancement of temozolomide (TMZ) delivery in the rat brain using a triolein emulsion.
MATERIALS AND METHODS
Rats were divided into the five groups as following: group 1 (negative control), group 2 (treated with triolein emulsion and TMZ 20 mg/kg), and group 3 (TMZ 20 mg/kg treatment without triolein), group 4 (treated with triolein emulsion and TMZ 10 mg/kg), and group 5 (TMZ 10 mg/kg treatment without triolein). Triolein emulsion was infused into the right common carotid artery. One hour later, the TMZ concentration was evaluated quantitatively and qualitatively using high-performance liquid chromatography (HPLC-MS) and desorption electrospray ionization mass spectrometry (DESI-MS) imaging, respectively. The concentration ratios of the ipsilateral to contralateral hemisphere in each group were determined and the statistical analysis was conducted using an unpaired -test.
RESULTS
Quantitatively, the TMZ concentration ratio of the ipsilateral to the control hemisphere was 2.41 and 1.13 in groups 2 and 3, and were 2.49 and 1.14 in groups 4 and 5, respectively. Thus, the TMZ signal intensities of TMZ in group 2 and 4 were statistically high in the ipsilateral hemispheres. Qualitatively, the signal intensity of TMZ was remarkably high in the ipsilateral hemisphere in group 2 and 4.
CONCLUSIONS
The triolein emulsion efficiently opened the blood-brain barrier and could provide a potential new strategy to enhance the therapeutic effect of TMZ. HPLC-MS and DESI-MS imaging were shown to be suitable for analyses of enhancement of brain TMZ concentrations.
Topics: Animals; Antineoplastic Agents, Alkylating; Blood-Brain Barrier; Brain; Chemistry, Pharmaceutical; Dose-Response Relationship, Drug; Drug Delivery Systems; Emulsions; Male; Rats; Rats, Sprague-Dawley; Temozolomide; Triolein
PubMed: 34747271
DOI: 10.1080/10717544.2021.1998247 -
International Journal of Nanomedicine 2022This work was aimed to develop a Curcuma oil-based self-nanoemulsifying drug delivery system (SNEDDS) 3D-printed polypills containing glimepiride (GMD) and rosuvastatin...
INTRODUCTION
This work was aimed to develop a Curcuma oil-based self-nanoemulsifying drug delivery system (SNEDDS) 3D-printed polypills containing glimepiride (GMD) and rosuvastatin (RSV) for treatment of dyslipidemia in patients with diabetes as a model for metabolic syndrome (MS).
METHODS
Compartmentalized 3D printed polypills were prepared and studied in streptozotocin/poloxamer induced diabetic/dyslipidemic rats. The pharmacokinetic parameters of GMD and RSV in the prepared polypills were evaluated. Blood glucose level, lipid profile, antioxidant, and biochemical markers activities were investigated. Also, histopathological examination of the liver and pancreas was carried out. The atherosclerotic index, the area of islets of Langerhans, and liver steatosis lesion scores were calculated.
RESULTS
The developed SNEDDS-loaded GMD/RSV polypills showed acceptable quality control characteristics with a high relative bioavailability of 217.16% and 224.28% for GMD and RSV, respectively, when compared with the corresponding non-SNEDDS pills. The prepared polypills showed dramatic lowering in blood glucose levels and substantial improvement in lipid profile and hepatic serum biomarkers as well as remarkable decrease in serum antioxidants in response to Poloxamer 407 intoxication. The prepared polypills decreased the risk of atherosclerosis and coronary disease by boosting the level of high-density lipoprotein and lowering both triglyceride and low-density lipoprotein. Microscopic examination showed normal hepatic sinusoids and high protection level with less detectable steatosis in the examined hepatocytes. Normal size pancreatic islets with apparently normal exocrine acini and pancreatic duct were also noticed.
CONCLUSION
This formulation strategy clearly shows the potential of the developed polypills in personalized medicine for treatment of patients with MS.
Topics: Administration, Oral; Animals; Blood Glucose; Emulsions; Humans; Lipids; Metabolic Syndrome; Nanoparticles; Nanotechnology; Particle Size; Printing, Three-Dimensional; Rats; Rosuvastatin Calcium; Solubility
PubMed: 35479768
DOI: 10.2147/IJN.S357356 -
Molecules (Basel, Switzerland) Oct 2020Polyphenols are micronutrients that are widely present in human daily diets. Numerous studies have demonstrated their potential as antioxidants and anti-inflammatory... (Review)
Review
Polyphenols are micronutrients that are widely present in human daily diets. Numerous studies have demonstrated their potential as antioxidants and anti-inflammatory agents, and for cancer prevention, heart protection and the treatment of neurodegenerative diseases. However, due to their vulnerability to environmental conditions and low bioavailability, their application in the food and medical fields is greatly limited. Nanoformulations, as excellent drug delivery systems, can overcome these limitations and maximize the pharmacological effects of polyphenols. In this review, we summarize the biological activities of polyphenols, together with systems for their delivery, including phospholipid complexes, lipid-based nanoparticles, protein-based nanoparticles, niosomes, polymers, micelles, emulsions and metal nanoparticles. The application of polyphenol nanoparticles in food and medicine is also discussed. Although loading into nanoparticles solves the main limitation to application of polyphenolic compounds, there are some concerns about their toxicological safety after entry into the human body. It is therefore necessary to conduct toxicity studies and residue analysis on the carrier.
Topics: Drug Delivery Systems; Emulsions; Liposomes; Metal Nanoparticles; Nanoparticles; Polyphenols
PubMed: 33050462
DOI: 10.3390/molecules25204613 -
Scientific Reports Dec 2021The aim of the present study was to formulate clindamycin (CLN) as a microsponge based gel to release the drug in a controlled manner and reduce the side effects in the...
The aim of the present study was to formulate clindamycin (CLN) as a microsponge based gel to release the drug in a controlled manner and reduce the side effects in the treatment of acne. Since this method requires poor water solubility of the drug to be loaded in particles, therefore, conversion of the hydrochloride salt to free base was done. By using an emulsion solvent diffusion method, we made six different formulations of microsponges containing CLN-free base by changing the proportions of polymer, emulsifier and the pH of the external phase. These formulations were studied for physical characterization and for drug- polymer interactions. The physical characterization showed that microsponge formulations coded by C5, C6 resulted in a better loading efficiency and production yield and their particle size was less than 30 µm. Scanning electron microscopy images showed the microsponges porous and spherical. C5, C6 microsponge formulation was prepared as gel in Carbopol and in vitro evaluated. The microsponge formulation gel C8 was found to be optimized. C8 released 90.38% of drug over 12 h and showed viscosity 20,157 ± 38 cp, pH of 6.3 ± 0.09 and drug content of 99.64 ± 0.04%. Fourier transform infrared spectroscopy and differential scanning calorimetry confirmed no significant interactions between excipients and drug.
Topics: Anti-Bacterial Agents; Clindamycin; Drug Delivery Systems; Emulsifying Agents; Emulsions; Gels; Polymers; Solubility
PubMed: 34857863
DOI: 10.1038/s41598-021-02826-7 -
Ultrasonics Sonochemistry May 2022To solve the problems of low bioavailability and unstable properties of Cinnamomum cassia Essential oil (CCEO), encapsulation technology was introduced as an effective...
To solve the problems of low bioavailability and unstable properties of Cinnamomum cassia Essential oil (CCEO), encapsulation technology was introduced as an effective means to improve its shortcomings. In this study, Cinnamomum cassia Essential oil nano-emulsion (CCEO-NE) was successfully synthesized by the oil-in-water method and characterized by standard analytical methods, including dynamic light scattering (DLS), Scanning electron microscopy (SEM), and Transmission electron microscopy (TEM). The results show that the synthesized CCEO is spherical, smooth in surface, and uniform in shape, with an average particle size of 221.8 ± 1.95 nm, which is amorphous. In this experiment, by simulating the digestion of CCEO-NE in the gastrointestinal tract, it was found that CCEO-NE was undigested in the oral cavity, mainly in the stomach, followed by the small intestine. By understanding the digestion of CCEO-NE, we can improve the potential of CCEO bioavailability in food and drug applications. In addition, through the study of ABTS and DPPH free radicals by CCEO and CCEO-NE, it was found that the antioxidant activity of CCEO-NE was more potent than that of CCEO. When the concentration of CCEO-NE and CCEO is 400 μg/mL, the DPPH free radical scavenging rate is 92.03 ± 0.548% and 80.46 ± 5.811%, respectively. In comparison, ABTS free radical scavenging rate is 90.35 ± 0.480% and 98.44 ± 0.170% when the concentration of CCEO- NE, and CCEO is 75 μg/mL, respectively. The antibacterial test shows that CCEO-NE can inhibit both Gram-positive and Gram-negative bacteria. Among them, CCEO-NE has a stronger antibacterial ability than CCEO, and the maximum inhibition zone diameter of CCEO can reach 15 mm, while that of CCEO-NE can reach 18 mm. Meanwhile, SEM and TEM showed that CCEO-NE treatment destroyed the ultrastructure of bacteria. Generally speaking, we know the situation of CCEO in the gastrointestinal tract. CCEO-NE has more potent antioxidant and antibacterial ability than CCEO. Our research results show that whey protein is an effective packaging strategy that can improve the effectiveness, stability, and even bioavailability of CCEO in various applications, including food and health care industries.
Topics: Anti-Bacterial Agents; Antioxidants; Cinnamomum aromaticum; Emulsions; Gram-Negative Bacteria; Gram-Positive Bacteria; Oils, Volatile
PubMed: 35472756
DOI: 10.1016/j.ultsonch.2022.106009