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Ampelopsin, one of the most common flavonoids, reported to possess numerous pharmacological activities and shows poor aqueous solubility. The purpose of this study was to enhance the dissolution rate and bioavailability of this drug by developing a novel delivery system that is microemulsion (ME) and to study the effect of microemulsion (ME) on the...
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... isolated from the tender stem and leaves of the plant species Ampelopsis grossedentata (Hand-Mazz) W. T. Wang, was one of the most common flavonoids (Figure 1). Ampelopsin was reported to possess numerous pharmaco- logical activities, such as anti-inflammatory, antimicrobial activity, relieving cough, antioxidation, antihypertension, hepatoprotective effect and anticarcinogenic effect [1][2][3][4]. ...
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Citations
... Piperine is an alkaloid derived from its oleoresin in black pepper, giving the bitter taste of P. longum L. and P. nigrum L. [13]. Recently, piperine has been found to be effective in the pigmentation mechanism as well as other biological activities [14]. A group of scientists from King's College London showed that basic alkaloid piperine and its synthetic derivatives stimulate skin pigmentation and are effective in restoring skin pigmentation [10]. ...
... To this end, Transcutol V R HP, a highly effective, non-toxic, biodegradable solubiliser, was used as a co-surfactant with an HLB value of 4.2 in our study. Similarly, several studies have been conducted using the co-surfactant and penetration enhancer properties of Transcutol V R [13][14][15]. Caprylic/ capric triglycerides are a fully saturated triglyceride cosmetic ingredient with superior emollient, easy spreadability and good user properties. It is derived entirely from vegetable sources and is preferred as an alternative to mineral or vegetable oils due to its high stability. ...
Background:
Eplerenone is a member of antihypertensives used individually or in combination with other medicines. Eplerenone exhibits poor solubility and is considered a class II drug.
Objective:
Increasing the solubility of eplerenone by using both liquid and solid self-emulsifying drug delivery system as an alternative to its marketed tablet product.
Methods:
Solubility studies of eplerenone were done with different oils, surfactants, and co-surfactants to determine which one has the highest solubility for eplerenone and determine the preference in the formulations of liquid self-emulsifying drug delivery system. The solidification process was carried out with the adsorption to solid carrier method. Optimal ratios of components were specified with pseudo-ternary phase diagram technique. Self-emulsifying drug delivery system formulations were characterized in terms of chemical interaction, droplet size/distribution, crystallization behaviors, and rheological evaluation. In vitro drug release studies were conducted and compared to pure drug and marketed product.
Results:
The solubility screening results showed high solubility of EPL in triacetin (11.99 mg/mL) as oil, Kolliphor®EL (≈ 2.65 mg/mL), and Tween®80 (≈ 1.91 mg/mL) as surfactant and polyethylene glycol 200 (PEG200) (≈ 8.50 mg/mL), dimethyl sulfoxide (≈ 7.57 mg/mL), Transcutol®P (≈ 6.03 mg/mL) as co-surfactant, respectively. Rheology studies revealed that liquid self-emulsifying drug delivery formulations exhibited non-Newtonian pseudoplastic flow.
Conclusion:
Solid self-emulsifying drug delivery systems prepared with Aerosil and Neusilin have shown tremendous improvement in terms of eplerenone dissolution by releasing the entire dose with boosted effect within 5 and 30 minutes respectively compared to the marketed product and pure eplerenone (p < 0.05).
... Rate conveyance of tests was estimated at 301 nm utilizing filtered water as blank. [17] Assay: ...
The objective of the present investigation was to develop and evaluate microemulsifying drug delivery system for improving the delivery of a BCS class II antidiabetic agent, glyburide (GLY). The solubility of glyburide in oils, surfactants and co-surfactants (Capmul MCM: Tween80: Span20) was evaluated to identify the components of the microemulsion. Pseudoternary phase diagrams diagram was utilized to identify the optimal excipient composition to formulate the microemulsion system and the area of microemulsion existence. Glyburide microemulsion was characterized by Refractive index, Optical profile of glyburide microemulsion was evaluated the pure drug in pH 7.4 buffers. The chemical stability of glyburide in microemulsion was determined as per the International Council for Harmonisation (ICH) guidelines.
... Microemulsions are water, oil, optically isotropic, thermodynamically stable [17] [18] [19], and low viscosity systems with a diameter of 10 to 100 nm, which form after mixing oil, water, and tensoactives [20] [21]. The tensoactive can be pure, mixed, or combined with other components, whose main function is reducing interfacial tension [22]. ...
Caffeine is an alkaloid present in a wide variety of plants. Currently the most consumed psychostimulant worldwide, its consumption is associated with several health benefits, including modulation of the innate and adaptive immune response, reduction of oxidative cellular stress, and decreased incidence of some cancers, including breast cancer. Breast cancer is the most common cause of cancer among women and the second leading cause of cancer death in women worldwide. The interaction between biomaterials and drugs has enabled a great advance in science for developing controlled drug delivery systems and has been used to treat numerous pathologies. This work aimed to evaluate the immunomodulatory effects of caffeine associated or not with polyethylene glycol adsorbed in microemulsion (MLP) on MCF-7 cells, pha-gocytic cells (MN), and coculture. For biological assays, ATCC (American Type Culture Collection, USA) cell lines of breast adenocarcinoma (MCF-7) and phagocytes (MN) obtained from voluntary donors were used. The cells (MN and MCF-7) and coculture were treated with caffeine and MLP and in-cubated for rheological characterization analyses: flow curve and viscosity, oxidative stress: superoxide anion assay (2 O −), and activity of the enzyme su-peroxide dismutase (Cu-Zn-SOD). Caffeine and MLP increased viscosity and blood and MCF-7 cells and affected the immunomodulation of oxidative stress metabolism of MN and MCF-7 cells treated with caffeine and associated caffeine to the MLP. These data suggest that caffeine is associated or not with MLP-induced immunomodulatory effects on MN phagocytes and
... Vibrational spectroscopy analysis in the infrared region showed that release rate in hydrogels is higher for hydrophilic than hydrophobic drugs [45]. The low water solubility of AMP may be an advantage, leading to a slower release of the drug release in PNVCL system and making longer the time of the drug action and reducing medication re-intake [46]. The influence of pH on drug release from PNVCL hydrogel systems was previously studied by Fallon et al. [47]. ...
This study aimed to evaluate the cytotoxicity and microbiological properties of poly (N-vinylcaprolactam)—PNVCL hydrogels containing flavonoids as intracanal medication for endodontic therapy. Antimicrobial activity of ampelopsin (AMP), isoquercitrin and rutin was determined against Enterococcus faecalis, Actinomyces israelii, Lactobacillus casei, Streptococcus mutans, and Fusobacterium nucleatum by the microdilution method. After synthesis and characterization by rheology, PNVCL hydrogels were loaded with AMP and controls calcium hydroxide (CH) and chlorhexidine (CHX), and determined the compounds release profile. PNVCL+AMP, PNVCL+CH, PNVCL+CHX were evaluated on multi-species biofilms and analyzed by Scanning Electron Microscopy (SEM) and Confocal Laser Scanning Microscopy (CLSM). Cytotoxicity was determined after fibroblasts exposure to serial dilutions of AMP and PNVCL hydrogel extracts. AMP was effective against all of the bacteria tested, especially against S. mutans, A. israelli and F. nucleatum. SEM and CLSM analysis showed that PNVCL + AMP caused a significant decrease and disorganization of multi-species biofilms and reduction of intracanal viable cells, superior to the other groups. AMP affected fibroblast viability at concentrations above 0.125 mg/mL, and extracts of PNVCL+AMP showed low cytotoxicity. In conclusion, PNVCL containing AMP demonstrated cytocompatibility and potent effect against multi-species biofilms and could be potential intracanal medication for endodontic purposes.
... However, nephrotoxic components of some herbal medicine including flavonoid glycosides was recently reviewed [115,116]. Since low bioavailability limits the pharmacologic efficacy [117], several preparations with better solubility or permeability have been identifies in vitro studies. These include microemulsion [118], nanoparticles [119], soluble cocrystals [120], nanoencapsulation [121], and solid dispersions and inclusion complex [13]. ...
The Coronavirus Disease 2019 (COVID-19) is a deThe unusual rates of morbidity and escalating degrees of mortality in nCV–2019
have compelled the WHO to declare public health emergency of international concern.
Vulnerability and transmissibility are particularly alarming in aged personnel, especially
those with underlying physiological ailments. Undoubtedly, the radiology sector plays the
pivot role in diagnostics and administration of epidemics, but owing to high pathogenic and
transmission potential of nCV–2019, there are several implications to deal with suspects.
Several findings of genomic evolutionary analyses endorse the divergence of nCV–2019
from the causative agents of MERS and SARS that have further perplexed the scientists
around the globe. Ever since the emergence, medical professionals are striving desperately
to discover a satisfactory cure. Presently, some anti–viral, traditional Chinese medications,
and plasma therapy are being employed on experimental basis; however, success rates
are still dismaying. As the immune system acts as the body’s first corp of defense against
viral invasions, the present review highlights the impact and its aggregates various dietary
components that serve as immunity boosters, i.e., vitamins, minerals, natural herbs,
spices, particular varieties of tea, drinks, Omega–3 fatty acids, and proteins. Diet therapy
is anticipated to minimize the nCV–2019 fatalities until the corresponding vaccine is
engineered.vastating global pandemic.
... it has been reported that DHM microemulsion systems include ordinary microemulsion preparation, Pickering emulsion, and self-emulsifying drug delivery system. Solanki et al. found that DHM microemulsion prepared with Capmul MCM as oil phase (DHM/Me-C), Cremophor eL as surfactant, and T-transcutol as co-surfactant would change from water-in-oil to bicontinuous phase with the addition of water, which regulated the dissolution and oral bioavailability of DHM (Solanki et al., 2012). Our group has prepared DHM microemulsions with different polarity oil phases and emulsifiers with different HLB values, during which we found that the selection of proper emulsifier and oil phase in the microemulsion system is very important. ...
Dihydromyricetin (DHM) is an important natural flavonoid that has attracted much attention because of its various functions such as protecting the cardiovascular system and liver, treating cancer and neurodegenerative diseases, and anti-inflammation effect, etc. Despite its great development potential in pharmacy, DHM has some problems in pharmaceutical applications such as low solubility, permeability, and stability. To settle these issues, extensive research has been carried out on its physicochemical properties and dosage forms to produce all kinds of DHM preparations in the past ten years. In addition, the combined use of DHM with other drugs is a promising strategy to expand the application of DHM. However, although invention patents for DHM preparations have been issued in several countries, the current transformation of DHM research results into market products is insufficient. To date, there is still a lack of deep research into the pharmacokinetics, pharmacodynamics, toxicology, and action mechanism of DHM preparations. Besides, preparations for combined therapy of DHM with other drugs are scarcely reported, which necessitates the development of dosage forms for this application. Apart from medicine, the development of DHM in the food industry is also of great potential. Due to its multiple effects and excellent safety, DHM preparations can be developed for functional drinks and foods. Through this review, we hope to draw more attention to the development potential of DHM and the above challenges and provide valuable references for the research and development of other natural products with a similar structure-activity relationship to this drug.
... The selection of the surfactant and co-surfactant was conducted on the basis of its emulsification ability with the selected oil, i.e., capmul MCM EP. The four surfactants screened were labrafac lipophile WL 1349, caproyl PGMS, cremophore and Tween 80. Amongst all, Tween 80 was selected, as it resulted in the formation of a clear emulsion with oil and had 75 ± 0.2% T. Tween 80 is a promising surfactant due to its high HLB value, i.e., 15 in comparison to the HLB value of capmul MCM EP, i.e., 5.5 due to which it exhibits a better emulsifying property that resulted in a decrease in interfacial tension, low entropy and rapid dispersion of oil globules in the aqueous phase that ultimately provided a stable microscopic oil in water nanoemulsion [62]. Since Tween 80 is non-ionic in nature, it results in a low magnitude of charge over the nanoparticles, which reduces the chances of agglomeration leading to stabilization of the formulation [63]. ...
The solid self-nanoemulsifying drug delivery system (s-SNEDDS) is a growing platform for the delivery of drugs via oral route. In the present work, tamoxifen (TAM) was loaded in SNEDDS with resveratrol (RES), which is a potent chemotherapeutic, antioxidant, anti-inflammatory and P-gp inhibitor for enhancing bioavailability and to obtain synergistic anti-cancer effect against breast cancer. SNEDDS were developed using capmul MCM as oil, Tween 80 as surfactant and transcutol-HP as co-surfactant and optimized by central composite rotatable design. Neusilin US2 concentration was optimized for adsorption of liquid SNEDDS to prepare s-SNEDDS. The developed formulation was characterized and investigated for various in vitro and cell line comparative studies. Optimized TAM-RES-s-SNEDDS showed spherical droplets of a size less than 200 nm. In all in vitro studies, TAM-RES-s-SNEDDS showed significantly improved (p ˂ 0.05) release and permeation across the dialysis membrane and intestinal lumen. Moreover, TAM-RES-s-SNEDDS possessed significantly greater therapeutic efficacy (p < 0.05) and better internalization on the MCF-7 cell line as compared to the conventional formulation. Additionally, oral bioavailability of TAM from SNEDDS was 1.63 folds significantly higher (p < 0.05) than that of combination suspension and 4.16 folds significantly higher (p < 0.05) than TAM suspension. Thus, findings suggest that TAM- RES-s-SNEDDS can be the future delivery system that potentially delivers both drugs to cancer cells for better treatment.
... A bicontinuous ME is made up of interconnected sponge-like domains of oil and water separated and subsequently stabilized by localized surfactants existing as surface interfaces [158,163,166]. ME are suitable for drug delivery due to their ease of preparation [167], unstable API protection [168], enhanced solubility of lipophilic API [169], controlled release of API [162], improved bioavailability via high absorption rates and enhanced penetration of biological membranes [170], improved shelf-life [171], and reduced intra-and inter-individual variability in the pharmacokinetics of an API [172]. The solubility of hydrophilic and lipophilic API may be improved by solubilization within globules and additional sites at the interfacial film [169,171]. ...
Neurodegenerative disorders including Alzheimer's, Parkinson's, and dementia are chronic and advanced diseases that are associated with loss of neurons and other related pathologies. Furthermore, these disorders involve structural and functional defections of the blood-brain barrier (BBB). Consequently, advances in medicines and therapeutics have led to a better appreciation of various pathways associated with the development of neurodegenerative disorders, thus focusing on drug discovery and research for targeted drug therapy to the central nervous system (CNS). Although the BBB functions as a shield to prevent toxins in the blood from reaching the brain, drug delivery to the CNS is hindered by its presence. Owing to this, various formulation approaches, including the use of lipid-based nanocarriers, have been proposed to address shortcomings related to BBB permeation in CNS-targeted therapy, thus showing the potential of these carriers for translation into clinical use. Nevertheless, to date, none of these nanocarriers has been granted market authorization following the successful completion of all stages of clinical trials. While the aforementioned benefits of using lipid-based carriers underscores the need to fast-track their translational development into clinical practice, technological advances need to be initiated to achieve appropriate capacity for scale-up and the production of affordable dosage forms.
... Several techniques are frequently used in the pharmaceutical industry for addressing low solubility by changing the physical, chemical, and physicochemical properties of the active ingredients [64]. Polymorphic forms, altering physicochemical properties, are interesting formulations for drug developers as they offer higher solubility than the original form [65]. Common physical techniques include spray-drying [66], micronization, emulsions [67,68], nanomilling [69], sono-crystallization [70] as well as chemical modifications such as solid dispersion [71], cocrystallization [72], cosolvent [73], salt formation [74], pH change [75], new solubilizer [76] and buffer solution [77] are utilized for solubility enhancement. The reduction of particle size is one of the most important techniques to improve bioavailability of poorly soluble drugs [78]. ...
In this study, we have directly incorporated nanographene oxide (nGO) into a hydrophobic drug for enhanced dissolution performance through an antisolvent technique. Apixaban (APX) drug composites were synthesized with nGO incorporation ranging from 0.8% - 2.0% concentration. It was observed that the nGO was successfully embedded without any changes to the original drug crystal structure or physical properties. Dissolution of the drug composites was evaluated using US Pharmacopeia Paddle Method (USP 42). The time needed to reach a 50% release (T50) reduced from 106 min to 24 min with the integration of 1.96% nGO in APX and the T80 also dropped accordingly. Alternatively, dissolution rate showed promising performance with increase in nGO concentration. Initial dissolution rate increased dramatically from 74 µg/min to 540 µg/min. Further, work done in intestinal media revealed T50 went from not dissolving to 79.0 minutes. Decreased lipophilicity or logP value and increased aqueous solubility are both accredited to hydrophilic nGO water dispersion, producing a hydrophilic channel into the drug crystal surfaces through intermolecular interaction. Additionally, physical, and chemical characterizations confirm that hydrophobic apixaban was successfully transformed into a hydrophilic composite, showing potential for this technology to improve dissolution rate of a model hydrophobic compound.
... The %Transmittance of the systems was found to be in range from 93.3 to 99.6. [17] Assay: ...
The aim of the present study was to develop and evaluate a microemulsifying drug delivery system to improve delivery of the glyburide an antidiabetic agent of BCS class II. (The solubility of glyburide in oils, surfactants and co-surfactants (oleic acid: transcutol-P: propylene glycol) was evaluated to identify the components of the microemulsion. The pseudo-terminal phase diagram was used to determine the optimal excipient composition for formulatingmicroemulsion system and microemulsion region of existence.Glyburide microemulsion was characterized by Refractive index, Optical Clarity, Assay, Dye solubility, Viscosity, Surface tension, pH, Drug Content, Polydispersity index, Drug loading, Entrapment efficiency, Particle size, Zeta Potential, Scanning Electron Microscopy (SEM), Differential scanning calorimetry measurements (DSC) and viscos¬ity. The in vitro dissolution profile of glyburide microemulsion was evaluated the pure drug in pH 7.4 buffers. The chemical stability of glyburide in microemulsion was determined as per the International Council for Harmonisation (ICH) guidelines.
