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Current Pharmaceutical Design 2017Most of the active pharmaceutical ingredients discovered recently in pharmaceutical field exhibits poor aqueous solubility that pose major problem in their oral... (Review)
Review
BACKGROUND
Most of the active pharmaceutical ingredients discovered recently in pharmaceutical field exhibits poor aqueous solubility that pose major problem in their oral administration. The oral administration of these drugs gets further complicated due to their short bioavailability, inconsistent absorption and inter/intra subject variability.
METHODS
Pharmaceutical emulsion holds a significant place as a primary choice of oral drug delivery system for lipophilic drugs used in pediatric and geriatric patients. Pharmacokinetic studies on nanoemulsion mediated drugs delivery approach indicates practical feasibility in regards to their clinical translation and commercialization.
RESULTS
This review article is to provide an updated understanding on pharmacokinetic and pharmacodynamic features of nanoemulsion delivered via oral, intravenous, topical and nasal route.
CONCLUSION
The article is of huge interest to formulation scientists working on range of lipophilic drug molecules intended to be administered through oral, intravenous, topical and nasal routes for vivid medical benefits.
Topics: Drug Administration Routes; Drug Delivery Systems; Emulsions; Humans; Nanostructures; Pharmaceutical Preparations
PubMed: 27908273
DOI: 10.2174/1381612822666161201143600 -
Current Topics in Medicinal Chemistry 2015Nasal delivery has become a growing area of interest for drug administration as a consequence of several practical advantages, such as ease of administration and... (Review)
Review
Nasal delivery has become a growing area of interest for drug administration as a consequence of several practical advantages, such as ease of administration and non-invasiveness. Moreover, the avoidance of hepatic first-pass metabolism and rapid and efficient absorption across the permeable nasal mucosa offer a promising alternative to other traditional administration routes, such as oral or parenteral delivery. In fact, nasal delivery has been proposed for a number of applications, including local, systemic, direct nose-to-brain and mucosal vaccine delivery. Nanoemulsions, due to their stability, small droplet size and optimal solubilization properties, represent a versatile formulation approach suitable for several administration routes. Nanoemulsions demonstrated great potential in nasal drug delivery, increasing the absorption and the bioavailability of many drugs for systemic and nose-to-brain delivery. Furthermore, they act as an active component, i.e. an adjuvant, in nasal mucosal vaccinations, displaying the ability to induce robust mucosal immunity, high serum antibodies titres and a cellular immune response avoiding inflammatory response. Interestingly, nanoemulsions have not been proposed for the treatment of local ailments of the nose. Despite the promising results in vitro and in vitro, the application of nanoemulsions for nasal delivery in humans appears mainly hindered by the lack of detailed toxicology studies to determine the effect of these formulations on the nasal mucosa and cilia and the lack of extensive clinical trials.
Topics: Administration, Intranasal; Emulsions; Humans; Nanostructures; Nasal Mucosa
PubMed: 25579345
DOI: 10.2174/1568026615666150108144655 -
Journal of Pharmaceutical Sciences Jul 2023The emulsion-based topical semisolid dosage forms present a high degree of complexity due to their microstructures which is apparent from their compositions comprising... (Review)
Review
The emulsion-based topical semisolid dosage forms present a high degree of complexity due to their microstructures which is apparent from their compositions comprising at least two immiscible liquid phases, often times of high viscosity. These complex microstructures are thermodynamically unstable, and the physical stability of such preparations is governed by formulation parameters such as phase volume ratio, type of emulsifiers and their concentration, HLB value of the emulsifier, as well as by process parameters such as homogenizer speed, time, temperature etc. Therefore, a detailed understanding of the microstructure in the DP and critical factors that influence the stability of emulsions is essential to ensure the quality and shelf-life of emulsion-based topical semisolid products. This review aims to provide an overview of the main strategies used to stabilize pharmaceutical emulsions contained in semisolid products and various characterization techniques and tools that have been utilized so far to evaluate their long-term stability. Accelerated physical stability assessment using dispersion analyzer tools such as an analytical centrifuge to predict the product shelf-life has been discussed. In addition, mathematical modeling for phase separation rate for non-Newtonian systems like semisolid emulsion products has also been discussed to guide formulation scientists to predict a priori stability of these products.
Topics: Emulsions; Emulsifying Agents; Viscosity
PubMed: 36966902
DOI: 10.1016/j.xphs.2023.03.014 -
ACS Nano May 2022Herein, we present the direct observation and quantification of a water-in-oil (w/o) emulsion, its destabilization, and the effect of additives on such processes at the...
Herein, we present the direct observation and quantification of a water-in-oil (w/o) emulsion, its destabilization, and the effect of additives on such processes at the nanoscale. This is achieved liquid phase transmission electron microscopy (LPTEM), wherein a small volume of emulsion is encapsulated against vacuum in its liquid state to allow observation of its initial morphology and its evolution over time at excellent spatial and temporal resolution. Emulsions of this class are useful for delivering payloads of materials insoluble in their delivery medium and are currently widely used across food science, pharmaceuticals, and environmental applications. However, their utility is inherently limited by their thermodynamic tendency to demulsify, eventually leading to bulk phase separation. This occurs several degradation mechanisms, operating at times collectively, and which are difficult to differentiate traditional ensemble methods (, light scattering), obscuring mechanistic nuances. LPTEM as a characterization technique has the potential to augment our understanding of emulsion behavior and improve performance and formulations. In this work, we also emphasize the importance of the included videographic Supporting Information data in demonstrating the behavior of the studied materials.
Topics: Emulsions; Water; Drug Compounding; Thermodynamics
PubMed: 35302741
DOI: 10.1021/acsnano.2c00199 -
Analytical Chemistry Dec 2017Automated and reproducible sample handling is a key requirement for high-throughput compound screening and currently demands heavy reliance on expensive robotics in...
Automated and reproducible sample handling is a key requirement for high-throughput compound screening and currently demands heavy reliance on expensive robotics in screening centers. Integrated droplet microfluidic screening processors are poised to replace robotic automation by miniaturizing biochemical reactions to the droplet scale. These processors must generate, incubate, and sort droplets for continuous droplet screening, passively handling millions of droplets with complete uniformity, especially during the key step of sample incubation. Here, we disclose an integrated microfluidic emulsion creamer that packs ("creams") assay droplets by draining away excess oil through microfabricated drain channels. The drained oil coflows with creamed emulsion and then reintroduces the oil to disperse the droplets at the circuit terminus for analysis. Creamed emulsion assay incubation time dispersion was 1.7%, 3-fold less than other reported incubators. The integrated, continuous emulsion creamer (ICEcreamer) was used to miniaturize and optimize measurements of various enzymatic activities (phosphodiesterase, kinase, bacterial translation) under multiple- and single-turnover conditions. Combining the ICEcreamer with current integrated microfluidic DNA-encoded library bead processors eliminates potentially cumbersome instrumentation engineering challenges and is compatible with assays of diverse target class activities commonly investigated in drug discovery.
Topics: Emulsions; Gene Library; High-Throughput Screening Assays; Microfluidic Analytical Techniques; Particle Size
PubMed: 29124927
DOI: 10.1021/acs.analchem.7b03070 -
PDA Journal of Pharmaceutical Science... 2022Pre-filled syringes have simplified parenteral administration of protein drugs. To ensure an easy and consistent movement of the plunger, the inner glass container...
Pre-filled syringes have simplified parenteral administration of protein drugs. To ensure an easy and consistent movement of the plunger, the inner glass container surface is typically siliconized. For bake-on siliconization, emulsions are sprayed on and heat treated. Due to the European Union regulation REACh ( the use of certain emulsion components, partially constituting the gold standard Liveo 365 35% Dimethicone NF Emulsion (Liveo 365), becomes restricted and Liveo 366 35% Dimethicone NF Emulsion (Liveo 366) has been introduced as an alternative. This change may affect the handling properties as well as the silicone layer formed. The purpose of these studies was to identify any differences that may influence the stability and safety of the final drug/device combination product to enable the use of the new emulsion. We compared silicone emulsions Liveo 365 and Liveo 366 and dilutions focusing on 1) their general physical stability, 2) the thermal degradation process of the emulsions and their components, and 3) the resulting silicone layer concerning chemistry, morphology, and functionality. The results were linked to the assessment of the final product regarding particle formation and short-term stability. A comparison of the emulsions Liveo 365 and Liveo 366 for bake-on siliconization is presented to support the transition of the latter as it becomes mandatory with REACh. Our studies show that the two emulsions do not significantly differ with respect to handling and stability, the resultant silicone layer characteristics as well as its functionality. We conclude that the transition to the new emulsion will not significantly impact the final product or the layer performance upon storage and with respect to particle formation.
Topics: Emulsions; Hot Temperature; Proteins; Silicones; Syringes
PubMed: 35365551
DOI: 10.5731/pdajpst.2020.012640 -
Physical Review. E Aug 2020We present a mechanistic model of drug release from a multiple emulsion into an external surrounding fluid. We consider a single multilayer droplet where the drug...
We present a mechanistic model of drug release from a multiple emulsion into an external surrounding fluid. We consider a single multilayer droplet where the drug kinetics are described by a pure diffusive process through different liquid shells. The multilayer problem is described by a system of diffusion equations coupled via interlayer conditions imposing continuity of drug concentration and flux. Mass resistance is imposed at the outer boundary through the application of a surfactant at the external surface of the droplet. The two-dimensional problem is solved numerically by finite volume discretization. Concentration profiles and drug release curves are presented for three typical round-shaped (circle, ellipse, and bullet) droplets and the dependency of the solution on the mass transfer coefficient at the surface analyzed. The main result shows a reduced release time for an increased elongation of the droplets.
Topics: Drug Delivery Systems; Drug Liberation; Emulsions; Kinetics; Models, Theoretical
PubMed: 32942448
DOI: 10.1103/PhysRevE.102.023114 -
Molecules (Basel, Switzerland) May 2022In the present study, chitosan-decorated multiple nanoemulsion (MNE) was formulated using a two-step emulsification process. The formulated multiple nanoemuslion was...
In the present study, chitosan-decorated multiple nanoemulsion (MNE) was formulated using a two-step emulsification process. The formulated multiple nanoemuslion was evaluated physiochemically for its size and zeta potential, surface morphology, creaming and cracking, viscosity and pH. A Franz diffusion cell apparatus was used to carry out in vitro drug-release and permeation studies. The formulated nanoemulsion showed uniform droplet size and zeta potential. The pH and viscosity of the formulated emulsion were in the range of and suitable for topical delivery. The drug contents of the simple nanoemulsion (SNE), the chitosan-decorated nanoemulsion (CNE) and the MNE were 71 ± 2%, 82 ± 2% and 90 ± 2%, respectively. The formulated MNE showed controlled release of itraconazole as compared with that of the SNE and CNE. This was attributed to the chitosan decoration as well as to formulating multiple emulsions. The significant permeation and skin drug retention profile of the MNE were attributed to using the surfactants tween 80 and span 20 and the co-surfactant PEG 400. ATR-FTIR analysis confirmed that the MNE mainly affects the lipids and proteins of the skin, particularly the , which results in significantly higher permeation and retention of the drug. It was concluded that the proposed MNE formulation delivers drug to the target site of the skin and can be therapeutically used for various cutaneous fungal infections.
Topics: Administration, Cutaneous; Chitosan; Emulsions; Skin; Skin Absorption; Surface-Active Agents
PubMed: 35630660
DOI: 10.3390/molecules27103183 -
International Journal of Pharmaceutics Jun 2017Emulsion technology has been utilized extensively in the pharmaceutical industry. This article presents a comprehensive review of the literature on an important... (Review)
Review
Emulsion technology has been utilized extensively in the pharmaceutical industry. This article presents a comprehensive review of the literature on an important subcategory of emulsions, microemulsions. Microemulsions are optically transparent, thermodynamically stable colloidal systems, 10-100nm diameter, that form spontaneously upon mixing of oil, water and emulsifier. This review is the first to address advantages and disadvantages, as well as considerations and challenges in multi-drug delivery. For the period 1 January 2011-30 April 2016, 431 publications related to microemulsion drug delivery were identified and screened according to microemulsion, drug classification, and surfactant types. Results indicate the use of microemulsions predominantly in lipophilic drug delivery (79.4%) via oil-in-water microemulsions and non-ionic surfactants (90%) for oral or topical administration. Cancer is the disease state most targeted followed by inflammatory diseases, microbial infections and cardiovascular disease. Key generalizations from this analysis include: 1) microemulsion formulation is largely based on trial-and-error despite over 1200 publications related to microemulsion drug delivery since their discovery in 1943; 2) characterization using methods including interfacial tension, droplet size, electrical conductivity, turbidity and viscosity may provide additional information for greater predictability; 3) microemulsion drug delivery publications arise primarily from China (27%) and India (21%) suggesting additional research opportunities elsewhere.
Topics: Administration, Oral; Administration, Topical; Chemistry, Pharmaceutical; Drug Delivery Systems; Emulsions; Humans; Surface-Active Agents
PubMed: 28495500
DOI: 10.1016/j.ijpharm.2017.05.005 -
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