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Colloids and Surfaces. B, Biointerfaces Sep 2020Emulsion formulations of essential oils are of major interest due to their relative biosafety, biocompatibility and good pharmacological potential. Their structural...
Emulsion formulations of essential oils are of major interest due to their relative biosafety, biocompatibility and good pharmacological potential. Their structural constituents (oil and water phase) facilitate ready solubilization of incorporated hydrophilic/lipophilic actives for their targeted delivery. In the present study, m5S cells were tested for their viability at various concentrations of clove oil and an alkyl polyglucoside emulsifier, viz., Montanov 202™. Thereafter, good cell viable concentrations of oil (10 %) and emulsifier (4%) were used at their optimised ratio (1:0.4) to formulate an oil in water emulsion using phase inversion technique followed by ultrasonication for particle size reduction. Gas chromatography-mass spectrometry (GC-MS) analysis of clove oil revealed eugenol (76.11 %) and eugenyl acetate (12.41 %) as major constituents. The formulated clove oil emulsion was then characterised with respect to its size, zeta potential, microscopic and thermal analysis and the presence of liquid crystals were observed in the same. It was further studied for its anti-inflammatory potential in female Wistar rats wherein topical treatment with the emulsion inhibited paw swelling induced by carrageenan model by 40-60% over 30-180 min compared to untreated animals. Similarly, the emulsion's wound healing potential was also significant with respect to wounds induced by both incision (wound breaking strength of 338.91 ± 5.02 g) and excision (95 % wound contraction by 16th day) model in these animals, with a re-epithelization period of 10.67 ± 1.67 days and results being comparable with diclofenac gel and neomycin cream (positive controls). Histopathology of the skin sections showed accelerated healing with early granular tissue and collagen formation in emulsion treated animals. It is hence envisaged that this clove oil emulsion can substitute chemical based topical products for anti-inflammatory and wound healing applications due to its biological constituents as well as because of the presence of liquid crystals in its formulation.
Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Carrageenan; Cell Proliferation; Cell Survival; Cells, Cultured; Clove Oil; Edema; Emulsions; Female; Mice; Oxidative Stress; Particle Size; Rats; Rats, Wistar; Surface Properties; Wound Healing
PubMed: 32442923
DOI: 10.1016/j.colsurfb.2020.111102 -
Pharmaceutical Development and... Jun 2017Transdermal drug delivery continues to attract considerable interest in the scientific community. However, due to the hindrance provided by the stratum corneum, it is... (Review)
Review
Transdermal drug delivery continues to attract considerable interest in the scientific community. However, due to the hindrance provided by the stratum corneum, it is not possible to deliver most medications in therapeutically significant amounts. One of the ways of increasing the penetration of drugs across the skin is through the use of microemulsions (MEs). This review focuses on the role of MEs in enhancing topical and transdermal drug delivery.
Topics: Administration, Cutaneous; Animals; Clinical Trials as Topic; Drug Delivery Systems; Emulsions; Humans; Oils; Pharmaceutical Preparations; Skin; Skin Absorption; Surface-Active Agents
PubMed: 26931453
DOI: 10.3109/10837450.2016.1148722 -
Drug Delivery Nov 2016Self-emulsifying drug delivery system (SEDDS) is an isotropic mixture of lipid, surfactant and co-surfactant, which forms a fine emulsion when comes in contact of an... (Review)
Review
Self-emulsifying drug delivery system (SEDDS) is an isotropic mixture of lipid, surfactant and co-surfactant, which forms a fine emulsion when comes in contact of an aqueous medium with mild agitation. SEDDS is considered as a potential platform for oral delivery of hydrophobic drug in order to overcome their poor and irregular bioavailability challenges. In spite of fewer advantages like improved solubility of drug, bypassing lymphatic transport etc., SEDDS faces different controversial issues such as the use of appropriate terminology (self-microemulsifying drug delivery system; SMEDDS or self-nanoemulsifying drug delivery system; SNEDDS), presence of high amount of surfactant, correlation of in vitro model to in vivo studies, lack of human volunteer study and effect of conversion of SEDDS to final administrable dosage form on pharmacokinetic behavior of the drug. In this review, potential issues or questions on SEDDS are identified and summarized from the pharmacokinetic point of view. Primarily this review includes the conflict between the influences of droplet size, variation in correlation between in vitro lipolysis or ex-vivo intestinal permeation and pharmacokinetic parameters, variation in in vivo results of solid and liquid SEDDS, and potential challenges or limitation of pharmacokinetic studies on human volunteers with orally administered SEDDS. In the past decades, hundreds of in vivo studies on SEDDS have been published. In the present study, only the relevant article on in vivo pharmacokinetic studies with orally administered SEDDS published in past 5-6 years are analyzed for an up to date compilation.
Topics: Administration, Oral; Animals; Biological Availability; Chemistry, Pharmaceutical; Drug Delivery Systems; Emulsifying Agents; Emulsions; Humans; Particle Size; Permeability; Surface-Active Agents
PubMed: 27685505
DOI: 10.1080/10717544.2016.1214990 -
Pharmaceutical Development and... Nov 2020Silymarin has a short half-life (4-6 hours) which leads to necessity of frequent administration. Besides, it suffers from intestinal degradation. Thus, our study aims...
Silymarin has a short half-life (4-6 hours) which leads to necessity of frequent administration. Besides, it suffers from intestinal degradation. Thus, our study aims to formulate encapsulated floating microspheres using different polymers as HPMC, EC and a blend of them. Emulsion solvent evaporation technique was applied for preparation of microspheres. Parameters considered during preparation are drug: polymer ratio and emulsifier concentration. Selected formulations were characterized by SEM and subjected for assessment by drug entrapment efficiency, buoyancy for 12 hr, drug release, kinetics of release and stability. bio-equivalence study was performed using albino rabbits. Formula F24 (treatment II) exhibited high % buoyancy (73.4), higher t (190.7 day), high C (1021.3 ng/ml) and T (6 h) with a significant difference between it and treatment I (Silymarin plus) after carrying out ANOVA study. Also formula F24 exhibited MRT (hr) equal 9.44 ± 0.03 and high relative bioavailability RB% (227%), which indicates promising microspheres that could be used for effective management of liver disease.
Topics: Animals; Chemistry, Pharmaceutical; Drug Delivery Systems; Drug Liberation; Emulsions; Microspheres; Polymers; Rabbits; Silymarin
PubMed: 32654568
DOI: 10.1080/10837450.2020.1795192 -
International Journal of Pharmaceutics Jun 2022In the present study, topical gel and emulsion gel were formulated using Acrylamide/ Sodium Acryloyldimethyl taurate copolymer (Sepineo P600) as a gelling agent, and...
In the present study, topical gel and emulsion gel were formulated using Acrylamide/ Sodium Acryloyldimethyl taurate copolymer (Sepineo P600) as a gelling agent, and their rheological attributes and physical stability were evaluated upon incorporation of API. Lidocaine, a free base drug (pK 7.92) was used as a model drug in all formulations. Medium- chain Triglycerides (MCT) was used as a dispersed phase to prepare the emulgel. Results show that the rheological properties of both gel and emulgel such as viscosity, elastic moduli and yield stress were significantly influenced by the pH of the topical formulations and API concentration. A lower pH (pH < pKa) leads to the increase in number of cationic species of lidocaine, which results in the weakening of the structure of the gel matrix by charge screening of polymer-polymer repulsions. Interactions between API and polymer chains through electrostatic attraction may play a major role in altering the rheology, which could potentially impact the physical stability against phase separation of the internal phase in emulsion gel samples. This study provides valuable insights into rheological behaviors of Sepineo P600 gel and emulgel which can be modified or tuned though the interplay of the API properties and critical formulation parameters such as pH. The tunable rheological properties with simpler manufacturing process make Sepineo P600 gel and emulsion gel very suitable systems for use in semisolid topical formulations.
Topics: Emulsions; Gels; Lidocaine; Polymers; Rheology; Viscosity
PubMed: 35569626
DOI: 10.1016/j.ijpharm.2022.121824 -
Zhongguo Zhong Yao Za Zhi = Zhongguo... Sep 2021This study was mainly based on the compatibility of Puerariae Lobatae Radix and Chuanxiong Rhizoma to prepare submicron emulsion and evaluated its physical and...
This study was mainly based on the compatibility of Puerariae Lobatae Radix and Chuanxiong Rhizoma to prepare submicron emulsion and evaluated its physical and pharmaceutical properties. Firstly, pseudo-ternary phase diagrams were drawn by dripping method which took Chuanxiong oil as the oil phase and the area of microemulsion region as the index. On this basis, suitable emulsifier and co-emulsifier were screened for the preparation of Chuanxiong oil submicron emulsion. Then, the formula realizing the largest oil loading was selected. Finally, puerarin substituted part of emulsifier and co-emulsifier to lower their content, so as to form puerarin-Chuanxiong oil submicron emulsion featuring the combination of medicine and adjuvant. Its particle size, zeta potential, centrifugal stability and storage stability were determined, and the in vitro drug release behavior was investigated by dialysis bag method, based on which the quality of the as-prepared submicron emulsion was evaluated comprehensively. The proposed method was proved feasible for the preparation of Chuanxiong oil submicron emulsion, which adopted polyoxyethylene castor oil(EL-40) as the emulsifier and was free from co-emulsifier. The formula of the maximum oil loading was found as Chuanxiong oil∶EL-40∶water 3∶7∶90. Further, puera-rin successfully replaced up to 10% of the emulsifier in submicron emulsion. Eventually, the optimal drug-loading formula was determined as puerarin∶Chuanxiong oil∶EL-40∶water 7∶30∶63∶900. The quality evaluation results of the as-prepared submicron emulsion demonstrated that the average emulsion droplet size was 333.9 nm, the PDI 0.26, and the zeta potential-10.12 mV. The submicron emulsion had a good centrifugal stability and did not present any instable phenomena such as delamination and precipitation during its standing still for 50 days. The evaluation of in vitro drug release behavior indicated that the submicron emulsion was capable of releasing the drug completely. The puerarin-chuanxiong oil submicron emulsion prepared in this study possessed a stable quality and to some extent increased the solubility of puerarin along with a sustained-release effect. This study provided ideas for the clinical application of puerarin.
Topics: Emulsions; Isoflavones; Particle Size; Solubility
PubMed: 34581044
DOI: 10.19540/j.cnki.cjcmm.20210412.303 -
International Journal of Cosmetic... Feb 2016In recent decades, considerable and continuous growth in consumer demand in the cosmetics field has spurred the development of sophisticated formulations, aiming at high... (Review)
Review
In recent decades, considerable and continuous growth in consumer demand in the cosmetics field has spurred the development of sophisticated formulations, aiming at high performance, attractive appearance, sensorial benefit and safety. Yet despite increasing demand from consumers, the formulator faces certain restrictions regarding the optimum equilibrium between the active compound concentration and the formulation base taking into account the nature of the skin structure, mainly concerning to the ideal penetration of the active compound, due to the natural skin barrier. Emulsion is a mixture of two immiscible phases, and the interest in nanoscale emulsion has been growing considerably in recent decades due to its specific attributes such as high stability, attractive appearance and drug delivery properties; therefore, performance is expected to improve using a lipid-based nanocarrier. Nanoemulsions are generated by different approaches: the so-called high-energy and low-energy methods. The global overview of these mechanisms and different alternatives for each method are presented in this paper, along with their benefits and drawbacks. As a cosmetics formulation is reflected in product delivery to consumers, nanoemulsion development with prospects for large-scale production is one of the key attributes in the method selection process. Thus, the aim of this review was to highlight the main high- and low-energy methods applicable in cosmetics and dermatological product development, their specificities, recent research on these methods in the cosmetics and consideration for the process selection optimization. The specific process with regard to inorganic nanoparticles, polymer nanoparticles and nanocapsule formulation is not considered in this paper.
Topics: Cosmetics; Emulsions; Nanostructures
PubMed: 26171789
DOI: 10.1111/ics.12260 -
Journal of Pharmaceutical and... Jan 2023Intravenous lipid emulsions (ILEs) are used for parenteral nutrition, providing a vital source of essential fatty acids and concentrated energy for patients who are...
Intravenous lipid emulsions (ILEs) are used for parenteral nutrition, providing a vital source of essential fatty acids and concentrated energy for patients who are unable to absorb nutrients via the digestive track. They are commonly used to treat local and non-local anesthetic toxicity, and lipophilic drug overdose. ILE are composed of natural lipids, and the composition of these natural lipids can be varied based on their source. The lipids are susceptible to hydrolytic degradation with time, resulting various lipid degradation products such as Lysophosphatidylcholines (LPs), affecting the actual composition of nutrients in the formulation. As a result, the identification and quantification of lipid components, including degradation products, in ILEs are crucial in quality control. In this study, lipids from different batches of ILE Intralipid® 20%, were separated and identified using a UHPLC-ESI-QTOF system and SimLipid® high throughput lipid identification software. Out of 47 lipids identified, 34 were phospholipids (PLs) and the others were triacylglycerols (TAGs). Most of the phospholipids detected were phosphatidylcholines (PC) and Lysophosphatidylcholines (LPC). A total of 9 LPCs, 18 PCs, 6 phosphoethanolamines (PEs), and 1 sphingomyelin (SM) were identified. The LPCs concentration changed with the manufacturing date and storage time. This UHPLC method enabled the identification and quantification of lipids and their decomposition products in complex ILE emulsion mixtures on a single 20-minute chromatographic run.
Topics: Humans; Fat Emulsions, Intravenous; Triglycerides; Lysophosphatidylcholines; Phospholipids; Emulsions; Parenteral Nutrition; Phosphatidylcholines
PubMed: 36274478
DOI: 10.1016/j.jpba.2022.115112 -
International Journal of Biological... Nov 2020Alginate or chitosan microparticles as drug loading system performed pH-responsiveness and biocompatibility, yet with the burst-release and limited encapsulation. In...
Alginate or chitosan microparticles as drug loading system performed pH-responsiveness and biocompatibility, yet with the burst-release and limited encapsulation. In order to improve the performance, herein, Pickering emulsion of chitosan-hydrophobic alginate nanocomposite (HSA-CS NCs) as the bio-stabilizer, was proposed as the drug-loading vehicle. Integrating the merits of HSA-CS and Pickering emulsion, such drug carrier of emulsion performed pH-response and biocompatibility from HSA-CS, and high loading capacity and rigid layer from Pickering emulsion, so as for the manipulated release behavior. With thorough investigation, via the various pH-response of HSA-CS nanocomposite in the continuous simulated gastrointestinal fluid, Pickering emulsion gradually released the loading drug (ibuprofen) out, performing the pH-triggered controlled-release behavior. Ibuprofen-loaded Pickering emulsions (30 mg/mL) released nearly none in SGF for 3 h, whereas in SIF, performed constant release in initial 5 h and continuous-release of 88.37% ibuprofen in 24 h with no drug-burst and high loading capacity, promisingly as the pH-responsive vehicle for drug delivery in oral route.
Topics: Alginates; Chitosan; Delayed-Action Preparations; Drug Carriers; Drug Liberation; Emulsions; Hydrophobic and Hydrophilic Interactions; Ibuprofen; Nanocomposites
PubMed: 32795582
DOI: 10.1016/j.ijbiomac.2020.08.092 -
Ceska a Slovenska Farmacie : Casopis... 2021Microparticles are widely used in myriad fields such as pharmaceuticals, foods, cosmetics, and other industrial fields. Compared with traditional methods for...
Microparticles are widely used in myriad fields such as pharmaceuticals, foods, cosmetics, and other industrial fields. Compared with traditional methods for synthesizing microparticles, microfluidic techniques provide very powerful platforms for creating highly controllable emulsion droplets as templates for fabricating uniform microparticles with advanced structures and functions. Microfluidic techniques can generate emulsion droplets with precisely controlled size, shape, and composition. A more precise preparation process brings an effective tool to control the release profile of the drug and introduces an easily accessible reproducibility. The paper gives information about basic droplet-based set-ups and examples of attainable microparticle types preparable by this method.
Topics: Emulsions; Microfluidic Analytical Techniques; Microfluidics; Reproducibility of Results
PubMed: 35114792
DOI: 10.5817/CSF2021-5-155