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ChemMedChem Jul 2021We present the development of surfactant-free, silica-free and fully biobased oil-in-water antimicrobial Pickering emulsions, based on the self-assembly of...
We present the development of surfactant-free, silica-free and fully biobased oil-in-water antimicrobial Pickering emulsions, based on the self-assembly of β-cyclodextrin and phytoantimicrobial oils (terpinen-4-ol or carvacrol). Undecylenic acid (UA), derived from castor oil, can be used as bio-based drug to treat fungal infection, but is less effective than petroleum-based drugs as azole derivatives. To maximize its antifungal potential, we have incorporated UA in fully biobased Pickering emulsions. These emulsions are effective against fungi, Gram-positive and Gram-negative bacteria. The carvacrol emulsion charged with UA is +390 % and +165 % more potent against methicillin-resistant S. aureus (MRSA), compared to UA and azole-based commercial formulations. Moreover, this emulsion is up to +480 % more efficient that UA ointment against C. albicans. Finally, remarkable eradication of E. coli and MRSA biofilms was obtained with this environmental-friendly emulsion.
Topics: Anti-Bacterial Agents; Antifungal Agents; Candida albicans; Castor Oil; Cymenes; Dose-Response Relationship, Drug; Emulsions; Escherichia coli; Methicillin-Resistant Staphylococcus aureus; Microbial Sensitivity Tests; Molecular Structure; Structure-Activity Relationship; Undecylenic Acids; beta-Cyclodextrins
PubMed: 33735940
DOI: 10.1002/cmdc.202100030 -
Pharmaceutical Nanotechnology Nov 2022In the present scenario, lipid-based novel drug delivery systems are the area of interest for the formulation scientist in order to improve the bioavailability of poorly... (Review)
Review
In the present scenario, lipid-based novel drug delivery systems are the area of interest for the formulation scientist in order to improve the bioavailability of poorly water-soluble drugs. A selfemulsifying drug delivery system (SEDDS) upon contact with the gastrointestinal fluid, forms an o/w emulsion. SEDDS has gained popularity as a potential platform for improving the bioavailability of the lipophilic drug by overcoming several challenges. The various advantages like improved solubility, bypassing lymphatic transport, and improvement in bioavailability are associated with SMEDDS or SNEDDS. The extent of the formation of stable SEDDS depends on a specific combination of surfactant, co-surfactant, and oil. The present review highlighted the different aspects of formulation design along with optimization and characterization of SEDDS formulation. It also gives a brief description of the various aspects of the excipients used in SEDDS formulation. This review also includes the conflict between types of SEDDS based on droplet size. There is an extensive review of various research regarding different solidification techniques used for SEDDS in the last three years.
Topics: Concurrent Review; Chemistry, Pharmaceutical; Drug Delivery Systems; Emulsions; Surface-Active Agents
PubMed: 35980062
DOI: 10.2174/2211738510666220817124744 -
European Journal of Drug Metabolism and... Mar 2023Many naturally available dietary molecules such as curcumin have not seen the market due to poor solubility, bioavailability, and photodegradability. Successful...
BACKGROUND AND OBJECTIVE
Many naturally available dietary molecules such as curcumin have not seen the market due to poor solubility, bioavailability, and photodegradability. Successful development of a lipid-based dry emulsion may overcome these issues and help in reaching the markets for natural dietary molecules such as curcumin. The current study aims to develop a dry emulsion formulation of curcumin using natural oil and evaluate its dissolution, photostability, pharmacokinetics, and anti-inflammatory activity.
METHODS
Dry emulsions were prepared using emu oil and corn oil as the lipid phase, Caproyl 90 and Cremophor RH 40 as surfactants, and dextrin as a hydrophilic carrier.
RESULTS
Microscopic studies showed the formation of spherical porous particles, and solid-state characterization using differential scanning calorimetry and powder X-ray diffraction showed the conversion of curcumin to an amorphous form. About 80% drug release was observed from formulation, whereas pure drug showed only 50% drug release in 30 min. In vivo pharmacokinetic studies showed fivefold improvement in the maximum concentration of curcumin in plasma (C) and sevenfold improvement in the area under the concentration-time curve of curcumin from emu oil formulation compared with pure curcumin. Significant differences were observed in the anti-inflammatory activity of curcumin dry emulsion and plain curcumin. Emu-oil-based formulations showed synergistic anti-inflammatory activity over corn-oil-based formulations with improved photostability.
CONCLUSION
The present study suggests that the dry emulsion may enhance the bioavailability with synergistic anti-inflammatory activity and photostability of curcumin when given orally.
Topics: Rats; Animals; Curcumin; Rats, Sprague-Dawley; Emulsions; Drug Delivery Systems; Anti-Inflammatory Agents; Biological Availability; Excipients; Solubility
PubMed: 36800055
DOI: 10.1007/s13318-023-00819-7 -
Molecules (Basel, Switzerland) Jun 2023Salidroside has been widely used in anti-tumor, cardiovascular, and cerebrovascular protection. However, there are few reports of its use for wound repair. Herein,...
Salidroside has been widely used in anti-tumor, cardiovascular, and cerebrovascular protection. However, there are few reports of its use for wound repair. Herein, salidroside inflammation-targeted emulsion gel and non-targeted emulsion gel were developed for wound repair. The inflammation-targeted emulsion gels showed an overall trend of better transdermal penetration and lower potential than non-targeted emulsion gels (-58.7 mV and -1.6 mV, respectively). The apparent improvement of the trauma surface was significant in each administration group. There was a significant difference in the rate of wound healing of the rats between each administration group and the model group at days 7 and 14. Pathological tissue sections showed that inflammatory cells in the epidermis, dermis, and basal layer were significantly reduced, and the granulation tissue was proliferated in the inflammation-targeted emulsion gel group and the non-targeted emulsion gel group. Regarding the expressions of EGF and bFGF, the expressions of bFGF and EGF in the tissues of the inflammation-targeted group at days 7, 14, or 21 were significantly higher than that of the non-targeted emulsion gel group and the model group, both of which were statistically significant compared with the model group ( < 0.05). These results demonstrated that salidroside has the potential as an alternative drug for wound repair.
Topics: Rats; Animals; Epidermal Growth Factor; Emulsions; Wound Healing; Inflammation; Gels
PubMed: 37446812
DOI: 10.3390/molecules28135151 -
Molecular Pharmaceutics Jul 2022An oil-in-water (o/w) nanoemulsion (NE), composed of oil globules, stabilized by a surfactant, and dispersed in an aqueous phase, is increasingly developed in complex...
An oil-in-water (o/w) nanoemulsion (NE), composed of oil globules, stabilized by a surfactant, and dispersed in an aqueous phase, is increasingly developed in complex drug formulation. Kinetically stable NEs are used to formulate hydrophobic drugs and typically provide higher dosage strengths and better content uniformity. However, little is known accurately about drug distribution in its multiphase solution, especially for the possible drug presence in the surfactant (s) phase, the interface layer between the dispersed oil (o) and the continuous water (w) phases. Here, high-resolution F quantitative NMR spectroscopy was applied directly and noninvasively on an o/w NE drug product containing difluprednate (DFPN). The well-resolved F peaks of DFPN depended on the shielding molecules in each phase, which revealed mass-balanced DFPN distribution in multiple phases of (w), (s), and (o) of NE globules at a quantity of 1.8 ± 0.1, 35 ± 2, and 59 ± 3% per labeled content, respectively. Furthermore, the dilution-dependent F peak line broadening and shift suggested a millisecond dynamic exchange between the NE and the less-noticed smaller but thermodynamically stable microemulsion (ME) globules in NE solution. The high-resolution NMR result revealed that the drug availability could be quickly achieved using an o/w NE formulation because of the drug multiphase distribution and the ME-assisted fast drug exchange among globules.
Topics: Emulsions; Hydrophobic and Hydrophilic Interactions; Surface-Active Agents; Water
PubMed: 35657300
DOI: 10.1021/acs.molpharmaceut.2c00025 -
Chemical Communications (Cambridge,... Feb 2022The role of poly(ε-caprolactone) (PCL) and its 3D scaffolds in tissue engineering has already been established due to its ease of processing into long-term degradable... (Review)
Review
The role of poly(ε-caprolactone) (PCL) and its 3D scaffolds in tissue engineering has already been established due to its ease of processing into long-term degradable implants and approval from the FDA. This review presents the role of high internal phase emulsion (HIPE) templating in the fabrication of PCL scaffolds, and the versatility of the technique along with challenges associated with it. Considering the huge potential of HIPE templating, which so far has mainly been focused on free radical polymerization of aqueous HIPEs, we provide a summary of how the technique has been expanded to non-aqueous HIPEs and other modes of polymerization such as ring-opening. The scope of coupling of HIPE templating with some of the advanced fabrication methods such as 3D printing or electrospinning is also explored.
Topics: Animals; Biocompatible Materials; Cell Proliferation; Emulsions; Free Radicals; Polyesters; Porosity; Printing, Three-Dimensional; Tissue Engineering; Tissue Scaffolds
PubMed: 35014993
DOI: 10.1039/d1cc04941k -
Comprehensive Reviews in Food Science... Nov 2020The development of lipid-based delivery systems has attracted much attention over the last years and a wide variety of strategies and formulations are currently... (Review)
Review
The development of lipid-based delivery systems has attracted much attention over the last years and a wide variety of strategies and formulations are currently available to encapsulate, protect, and target delivery of bioactive and functional lipophilic constituents within the food and pharmaceutical industries. Waxes are crystalline lipid material, consisting of a complex mixture of long-chain fatty acids and fatty alcohols, hydrocarbons, aldehydes, and ketones and show great promises as constituents of carrier systems. Most of waxes are classified under food-grade category and show high availability at a low cost. This review article has provided a comprehensive summary of research on major carriers containing wax as one of the main constituents, including solid lipid nanoparticles, nanostructured lipid carriers, oleogels, and Pickering emulsions, with a focus on their food applications. The physical and chemical nature of natural waxes are described in the first while the second part deals with the structure, formulation, main methods of preparation, characterization, and finally utilization of each type of wax-based delivery system for specific food applications.
Topics: Drug Delivery Systems; Emulsions; Lipids; Nanostructures; Organic Chemicals; Waxes
PubMed: 33337056
DOI: 10.1111/1541-4337.12614 -
Critical Reviews in Food Science and... 2023In contrast to conventional particles that have isotropic surfaces, Janus ("two-faced") particles have anisotropic surfaces, which leads to novel physicochemical... (Review)
Review
In contrast to conventional particles that have isotropic surfaces, Janus ("two-faced") particles have anisotropic surfaces, which leads to novel physicochemical properties and functional attributes. Janus particles with differing compositions, structures, and functional attributes have been prepared using a variety of fabrication methods. Depending on their composition, Janus particles have been classified as inorganic, polymeric, or polymeric/inorganic types. Recently, there has been growing interest in preparing Janus particles from biological macromolecules to meet the demand for a more sustainable and environmentally friendly food and pharmaceutical supply. At interfaces, Janus particles exhibit the characteristics of both surfactants and Pickering stabilizers, and so their behavior can be described using adsorption theories developed to describe these surface-active substances. Research has highlighted several potential applications of Janus particles in food and medicine, including emulsion formation and stabilization, toxin detection, antimicrobial activity, drug delivery, and medical imaging. Nevertheless, further research is needed to design and fabricate Janus particles that are suitable as functional ingredients in the food and biomedicine industries.
Topics: Multifunctional Nanoparticles; Emulsions; Drug Delivery Systems; Polymers; Surface-Active Agents
PubMed: 35475710
DOI: 10.1080/10408398.2022.2067831 -
European Journal of Pharmaceutical... May 2022Critically ill and anesthetized patients commonly receive life-sustaining medications by pump-driven continuous intravenous infusion. Microinfusion refers to delivering...
Critically ill and anesthetized patients commonly receive life-sustaining medications by pump-driven continuous intravenous infusion. Microinfusion refers to delivering concentrated drugs with low flow carriers to conserve fluid administration. Most infused medications are water-soluble. Delivery onset lag times have been identified for microinfusions of water-soluble drugs or experimental surrogates. Drugs may be formulated as emulsions. Initiation of emulsion microinfusions has not been described. We tested in vitro the hypothesis that an emulsion's physical characteristics would influence its microinfusion delivery onset. We adapted an established in vitro model of pump-driven continuous intravenous microinfusion to compare the delivery of methylene blue as a surrogate for water-soluble drugs and a 10% lipid emulsion as a surrogate for a drug formulated as an emulsion. The drug surrogates joined the carrier with carrier flow vertically upwards, vertically downwards or horizontally. We measured the times to 5%, 50% and 95% of plateau delivery. Emulsion entry into a vertical (upwards) carrier flow resulted in a rapid initial emulsion delivery exceeding predictions of delivery models. Emulsion entry into both horizontal and vertical (downwards) carrier flows resulted in long lag times to steady state. Methylene blue delivery was unaffected by carrier flow orientation. Initiating microinfusion emulsion delivery with upward flow can result in a relative bolus, whereas long delivery lags would be expected with horizontal or downwards flow. An emulsion might carry a high potency drug having significant physiologic effects, e. g. clevidipine. Unrecognized, differences in initial emulsion delivery kinetics depending on carrier flow orientation may have clinical implications for both efficacy and safety.
Topics: Administration, Intravenous; Drug Delivery Systems; Emulsions; Equipment Design; Humans; Infusions, Intravenous
PubMed: 35227840
DOI: 10.1016/j.ejps.2022.106154 -
Biomaterials Science Jun 2023Hyperlipidemia is a lipid metabolism disorder that requires long-term and daily medication. Leonurine (Leo), an active alkaloid derived from , can effectively ameliorate...
Hyperlipidemia is a lipid metabolism disorder that requires long-term and daily medication. Leonurine (Leo), an active alkaloid derived from , can effectively ameliorate lipid profiles in mammals and serve as a candidate antihyperlipidemic agent for clinical applications. In this paper, poly(lactic--glycolic acid) (PLGA) microsphere (MP)-based drug delivery platforms were for the first time employed for hyperlipidemia management by encapsulating leonurine nanocrystals (Leo-nano) by a modified solid-in-oil-in-water (S/O/W) double emulsion-solvent emulsion technique. The optimal formulation (Leo-nano@MP) was characterized by a high drug loading and encapsulation efficiency of 19.90 ± 0.82% and 79.62 ± 3.57%, respectively, which followed first-order drug release kinetics over 20 days . Interestingly, Leo-nano@MP exhibited a unique morphology with a condensed surface yet a porous internal structure, which potentially contributed to the enhanced drug loading and release properties. Furthermore, subcutaneous injection of Leo-nano@MP every two weeks significantly ameliorated the lipid profiles and alleviated liver and kidney injury in HFD-fed rats in comparison with daily administration of free Leo. Besides, no abnormalities in the heart, lung, spleen, and skin tissues at injection sites were observed. In summary, Leo-nano@MP with enhanced therapeutic efficacy, reduced administration frequency, and good biosafety constitutes a promising sustained-release platform for hyperlipidemia management.
Topics: Rats; Animals; Emulsions; Microspheres; Hyperlipidemias; Nanoparticles; Lipids; Particle Size; Delayed-Action Preparations; Mammals
PubMed: 37248852
DOI: 10.1039/d3bm00211j