Since the discovery of nanomedicine-based drug delivery carriers such as nanoparticles, liposomes, and self-nanoemulsifying drug delivery systems (SNEDDS), enormous progress has been achieved in the ...field of innovative active biomolecule drug delivery systems ....
A growing tendency toward the discovery and use of natural bioactive compounds that are the least harmful, have the fewest side effects, and are the most natural for the human body has been noticed ...during the past few decades ...
Recently caffeine has been investigated for the treatment of various types of cancers upon oral administration. There is also some evidence that dermally applied caffeine can protect the skin from ...skin cancer caused by sun exposure. Therefore nanoemulsion formulation of caffeine for transdermal drug delivery was developed and evaluated in the present investigation. Different w/o nanoemulsion formulations of caffeine were prepared by oil phase titration method. Thermodynamically stable nanoemulsions were characterized for morphology, droplet size, viscosity and refractive index. The
in
vitro skin permeation studies were performed on Franz diffusion cell using rat skin as permeation membrane. The
in vitro skin permeation profile of optimized formulation was compared with aqueous solution of caffeine. Significant increase in permeability parameters was observed in nanoemulsion formulations (
P
<
0.05) as compared to aqueous solution of caffeine. The steady-state flux (
J
ss) and permeability coefficient (
K
p) for optimized nanoemulsion formulation (C12) were found to be 147.55
±
8.21
μg/cm
2/h and 1.475
×
10
−2
±
0.031
×
10
−2
cm/h, respectively. Enhancement ratio (
E
r) was found to be 17.37 in optimized formulation C12 compared with other formulations. Overall these results suggested that w/o nanoemulsions are good carriers for transdermal delivery of caffeine.
In this study, the solubility, molecular interactions and mixing thermodynamic properties of a poorly water soluble bioactive compound piperine in twelve different pure solvents namely “water, ...methanol, ethanol, isopropyl alcohol (IPA), ethylene glycol (EG), propylene glycol (PG), 1-butanol, 2-butanol, ethyl acetate (EA), dimethyl sulfoxide (DMSO), polyethylene glycol-400 (PEG-400) and 2-(2-ethoxyethoxy) ethanol Transcutol®” were evaluated. The solubility of piperine was determined at temperatures “T=298.2K to 318.2K” and pressure “p=0.1MPa”. The experimental solubility values of piperine were determined using a static equilibrium method by high-performance liquid chromatography at 254nm. The solubility data of piperine obtained in this study was regressed using “van't Hoff and Apelblat models” with root mean square deviation values of <5.0%. The solubilities of piperine in mole fraction were obtained maximum in Transcutol (9.17×10−2) followed by PEG-400 (7.88×10−2), DMSO (3.59×10−3), 2-butanol (2.25×10−2), 1-butanol (2.20×10−2), IPA (1.82×10−2), EA (1.54×10−2), PG (1.47×10−2), ethanol (1.34×10−2), methanol (7.91×10−3), EG (6.70×10−3) and water (1.52×10−5) at “T=318.2K”. Based on the results of activity coefficient, the solute-solvent interaction was seen maximum in piperine-Transcutol and piperine-PEG-400 in comparison with other solute-solvent combination studied. Mixing thermodynamic properties of piperine were determined by activity coefficient model and results indicated spontaneous and entropy-driven dissolution of piperine in most of the pure solvents studied.
•Solubility of piperine in twelve different pure solvents was determined.•The mole fraction solubilities of piperine were obtained maximum in Transcutol.•Experimental solubilities of piperine were correlated well with calculated ones.•The dissolution of piperine was recorded as spontaneous and entropy-driven.
Objective
The current studies were undertaken to enhance dissolution and bioavailability/pharmacokinetic profile of a newly approved anticancer drug ibrutinib (IBR) via encapsulation of drug into ...self‐nanoemulsifying drug delivery system (SNEDDS).
Methods
Various SNEDDS formulations of IBR were developed by aqueous phase titration method using Capryol‐PGMC (oil phase), Tween‐20 (surfactant), Carbitol (cosurfactant) and water (aqueous phase). Developed SNEDDS of IBR was evaluated in vitro for various physicochemical properties and drug release profile.
Key findings
Based on lowest droplet size (28.7 ± 3.2 nm), least polydispersity (0.123), optimal values of zeta potential (−32.8 mV) and refractive index (1.336), highest % transmittance (98.7 ± 0.2%), highest drug release profile via dialysis membrane (98.9 ± 8.2% after 48 h) and the presence of lowest concentration of Capryol‐PGMC (12% w/w), SNEDDS I1 was selected for in‐vivo pharmacokinetic/bioavailability studies in female Wistar rats. In‐vivo pharmacokinetic studies in rats showed that optimized SNEDDS I1 controlled the absorption of IBR compared with IBR suspension. The bioavailability of IBR from optimized SNEDDS I1 was enhanced around 2.64 times in comparison with IBR suspension.
Conclusion
These results indicated the potential of developed SNEDDS as an alternative drug delivery system for IBR to enhance its bioavailability and anticancer efficacy.
The solubility values, various Hansen solubility parameters (HSPs) and thermodynamic behavior of emtricitabine (ECT) in twelve different pure solvents (PS) were estimated using various experimental ...as well as computational methods. Experimental solubility values (
) of ECT in twelve different PS were obtained at
= 298.2 K to 318.2 K and
= 0.1 MPa. The
values of ECT were correlated by "van't Hoff, Apelblat and Buchowski-Ksiazaczak
models". Various HSPs for ECT and twelve different PS were also calculated using "HSPiP software". The
values of ECT were estimated maximum in polyethylene glycol-400 (PEG-400; 1.41 × 10
), followed by ethylene glycol, Transcutol-HP, propylene glycol, methanol, water, isopropanol, ethanol, 1-butanol, dimethyl sulfoxide, 2-butanol and EA (1.28 × 10
) at
= 318.2 K. "Apparent thermodynamic analysis" showed an "endothermic and entropy-driven dissolution" of ECT. Overall, PEG-400 was found as the best/ideal solvent for solubility/miscibility of ECT compared to other solvents studied.
Phoenix dactylifera
(date palm) is a member of the genus
Phoenix
belonging to family Arecaceae. It is widely cultivated for its edible fruits and kernels. Dates have been used for both dietary ...purposes as well as for their phytomedicinal impacts against the variety of diseases. Date fruits are rich in alkaloids, protein, carbohydrate, fatty acid (linoleic, lauric, palmitic, and stearic acid), carotenoids, vitamins, polyphenolic compounds, flavonoids, and tannins along with different types of nutrients like potassium, calcium, magnesium, and phosphorus. Due to the presence of the variety of phytochemicals, they have greater impact on human health. They have strong antioxidant potential. It has been proposed now as a potential source of several unique medical and industrial products. In literature, much information is available on botanical descriptions, agriculture technology, and utilization in therapeutic intervention, but a little description is accessible on phytochemical relevance, formulation strategies, nutritional impact, and bioprocess technology. Therefore, the present review provides comprehensive information on the phytochemical relevance, pharmacology/bioactivity, pharmaceutical impact, their scope in bioprocess technology and nutraceutical values of date palm. According to all collected information, every portion of the plant has some beneficial properties that can serve as a source of medicine and nutraceutical.
The solubilization, solution thermodynamics, solvation behavior and Hansen solubility parameters (HSPs) of an anti-inflammatory medicine flufenamic acid (FFA) in various Carbitol + water mixtures ...were evaluated in this study. The experimental solubility of FFA in mole fraction (xe) was measured at T = 298.2–318.2 K and p = 0.1 MPa using a static equilibrium method. The xe values of FFA in various Carbitol + water mixtures were correlated with van’t Hoff, Apelblat, Yalkowsky–Roseman, Jouyban–Acree and Jouyban–Acree–van’t Hoff models. All the studied models showed good correlation with mean error values of less than 2%. The xe value of FFA was found to increase significantly with the increase in temperature and Carbitol mass fraction in all Carbitol + water mixtures evaluated. The maximum and minimum xe values of FFA were recorded in pure Carbitol (2.81 × 10−1) at T = 318.2 K and pure water (5.80 × 10−7) at T = 298.2 K, respectively. Moreover, the HSP of FFA was found to be more closed with that of pure Carbitol, indicating the maximum solubility of FFA in pure Carbitol. The estimated values of activity coefficients showed higher molecular interactions in FFA–Carbitol combinations compared with FFA–water combinations. Thermodynamic studies indicated an endothermic and entropy-driven dissolution of FFA in all Carbitol + water mixtures. The solvation behavior of FFA was observed as enthalpy driven in all Carbitol + water combinations evaluated.
The solubility data of poorly soluble anti-inflammatory drug flufenamic acid (FFA) are scarce in literature. Therefore, in the current study, the solubility of FFA in eleven different neat solvents ...including “water, methanol, ethanol, isopropanol (IPA), ethylene glycol (EG), propylene glycol (PG), 1-butanol, 2-butanol, dimethyl sulfoxide (DMSO), polyethylene glycol-400 (PEG-400) and Transcutol®” was measured and correlated at temperatures “T=298.2K to 318.2K” and pressure “p=0.1MPa”. The solubilities of FFA in mole fraction were measured using a static equilibrium method and correlated with “van't Hoff and Apelblat equations”. The mole fraction solubilities of FFA were obtained maximum in DMSO (2.86×10−1), followed by Transcutol (2.78×10−1), 2-butanol (1.79×10−1), 1-butanol (1.77×10−1), IPA (1.44×10−1), ethanol (1.12×10−1), methanol (6.29×10−2), PEG-400 (6.16×10−2), EG (1.20×10−2), PG (1.81×10−2) and water (1.60×10−6) at “T=318.2K” and similar trends were also recorded at each temperature studied. Activity coefficients were also calculated in order to evaluate the molecular interactions between solute and solvent molecules and results showed higher solute-solvent molecular interactions in FFA-DMSO, FFA-Transcutol, FFA-2-butanol, FFA-1-butanol, FFA-IPA and FFA-ethanol in comparison with other solute-solvent combinations. “Apparent thermodynamic analysis” showed an “endothermic and entropy-driven dissolution” of FFA in all neat solvents studied.
Display omitted
•Solubility of flufenamic acid (FFA) in different neat solvents was determined.•The mole fraction solubilities of FFA were obtained maximum in DMSO.•Solubilities of FFA were correlated well with calculated ones.•The dissolution of FFA was obtained as endothermic and entropy-driven.
This study demonstrated improved transdermal delivery of rifampicin-loaded cationic nanoemulsion gel to treat systemic and cutaneous tuberculosis using capmul, labrasol, and acconon, which exert ...anti-
activities. This approach enhanced drug permeation across the skin, increased therapeutic efficacy, and reduced dose-related side effects.
Design Expert
was used to optimize formulations (S
ratio and capmul as independent factors), which were prepared using a slow spontaneous titration method. The optimized nanoemulsion was incorporated into carbopol gel to allow for topical application and comparative assessments. Nanoemulsions and gels were evaluated for size, size distribution, shape, zeta potential, percent spread, viscosity, in vitro hemolysis, in vitro release, and ex vivo skin permeation and deposition. A mechanistic evaluation was performed using scanning electron microscopy. Furthermore, in vivo pharmacokinetic and irritation studies were performed.
The optimized cationic nanoemulsion (OCNE-1) was characterized by small particle size (≤100 nm), had optimal viscosity, percent spread, zeta potential, and percent drug release, and was hemocompatible. The OCNE-1T gel exhibited higher permeation flux (51.32 ± 0.5 µg/cm
hr), permeation coefficient (2.566 ± 0.08 cm/hr), drug deposition (994.404 µg/cm
), and enhancement ratio (7.16) than those of the OCNE-1 nanoemulsion or drug solution. Scanning electron microscopy was used to characterize the mechanism of enhanced permeation. An In vivo study showed that the C
and area under the curve following transdermal application were 4.34- and 4.74-fold higher than those following oral administration.
Transdermal delivery of rifampicin could be a promising alternative to conventional approaches to treat systemic and local tuberculosis, and other bacterial infections.
PDF
