The present research work is designed to prepare and optimize butenafine (BT) loaded poly lactic co glycolic acid (PLGA) nanoparticles (BT-NPs). BT-NPs were prepared by emulsification probe ...sonication method using PLGA (A), PVA (B) as polymer and stabilizer, respectively. The optimum composition of BT-NPs was selected based on the point prediction method given by the Box Behnken design software. The optimized composition of BT-NPop showed a particle size of 267.21 ± 3.54 nm with an entrapment efficiency of 72.43 ± 3.11%. The optimum composition of BT-NPop was further converted into gel formulation using chitosan as a natural polymer. The prepared topical gel formulation (BT-NPopG) was further evaluated for gel characterization, drug release, permeation study, irritation, and antifungal studies. The prepared BT-NPopG formulation showed optimum pH, viscosity, spreadability, and drug content. The release and permeation study results revealed slow BT release (42.76 ± 2.87%) with significantly enhanced permeation across the egg membrane. The irritation study data showed negligible irritation with a cumulative score of 0.33. The antifungal study results conclude higher activity than marketed as well as pure BT. The overall conclusion of the results revealed BT-NPopG as an ideal delivery system to treat topical fungal infection.
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.
The investigation aimed to evaluate the favourable effects of rosinidin in lipopolysaccharide (LPS)-induced learning and memory impairment in rats. Adult Wistar rats (150-200 g) were segregated ...equally into four different groups and treated as below: Group 1 (normal) and Group 2 (LPS control) were administered orally with 3 mL of 0.5% SCMC (vehicle); Group 3 and Group 4 were test groups and orally administered with rosinidin lower dose (10 mg/kg) and higher dose 20 mg/kg. Daily, 1 h post-offer mentioned treatments, Group 1 animals were injected with normal saline (i.p.) and groups 2-4 were treated with 1 mg/kg/day of LPS. This treatment schedule was followed daily for 7 days. During the treatment, schedule rats were evaluated for spontaneous locomotor activity, memory, and learning abilities. The biochemical assessment was carried out of acetylcholine esterase (AChE), endogenous antioxidants (GSH, SOD, GPx, and catalase), oxidative stress marker MDA, neuroinflammatory markers (IL-6, IL-1β, TNF-α, and NF-κB), and BDNF. LPS-induced reduced spontaneous locomotor activity and memory impairment in the animals. Moreover, LPS reduced GSH, SOD, GPx, and catalase levels; altered activities of AChE; elevated levels of MDA, IL-6, IL-1β, TNF-α, and NF-κB; and attenuated the levels of BDNF in brain tissue. Administration of rosinidin to LPS-treated animals significantly reduced LPS-induced neurobehavioral impairments, oxidative stress, neuroinflammatory markers, and reversed the Ach enzyme activities and BDNF levels towards normal. Results demonstrated that rosinidin attenuates the effects of LPS on learning memory in rats.
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.
Sustainable supply chain management (SSCM) has been a tough challenge for developing economies like Saudi Arabia. Implementation of SSCM practices in the manufacturing industry has been prone to ...multiple risk factors that need to be identified, evaluated, and prioritized especially considering the dynamics of the manufacturing industry in a developing economy. Moreover, it is also imperative to trace out feasible and sustainable strategies to overcome the risks to SSCM practices adoption. This study serves this purpose and identifies, evaluates, prioritizes the risk factors, sub-factors, and strategies to overcome these risk factors in the implementation of SSCM practices in the manufacturing industry in Saudi Arabia. An integrated multi-criteria decision analysis approach by combining fuzzy AHP and fuzzy WASPAS methods is employed for the analyses. The fuzzy AHP analysis results show that economic risks are dominant risks followed by the managerial policy risks and environmental risks in implementing SSCM. Industrial emissions are the leading risk factors in the overall ranking of the sustainable supply chain sub-risk factors followed by market dynamics, management policy failures, financial constraints, and credit uncertainty. While evaluating the sustainable supply chain strategies using fuzzy WASPAS, it is concluded that commitment and support of top, middle, and lower level management is the most pivotal strategy to deal with the risks to SSCM in Saudi Arabia followed by establishing environmental policies and goals to adopt SSCM, and provision of the financial resources and subsidies.
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.
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•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.
Cancer is a group of disorders characterized by uncontrolled cell growth that affects around 11 million people each year globally. Nanocarrier-based systems are extensively used in cancer imaging, ...diagnostics as well as therapeutics; owing to their promising features and potential to augment therapeutic efficacy. The focal point of research remains to develop new-fangled smart nanocarriers that can selectively respond to cancer-specific conditions and deliver medications to target cells efficiently. Nanocarriers deliver loaded therapeutic cargos to the tumour site either in a passive or active mode, with the least drug elimination from the drug delivery systems. This review chiefly focuses on current advances allied to smart nanocarriers such as dendrimers, liposomes, mesoporous silica nanoparticles, quantum dots, micelles, superparamagnetic iron-oxide nanoparticles, gold nanoparticles and carbon nanotubes, to list a few. Exhaustive discussion on crucial topics like drug targeting, surface decorated smart-nanocarriers and stimuli-responsive cancer nanotherapeutics responding to temperature, enzyme, pH and redox stimuli have been covered.
The solubility values and thermodynamic parameters of a natural phytomedicine/nutrient piperine (PPN) in Transcutol-HP (THP) + water combinations were determined. The mole fraction solubilities (
) ...of PPN in THP + water combinations were recorded at
= 298.2-318.2 K and
= 0.1 MPa by the shake flask method. Hansen solubility parameters (HSPs) of PPN, pure THP, pure water and THP + water mixtures free of PPN were also computed. The
values of PPN were correlated well with "Apelblat, Van't Hoff, Yalkowsky-Roseman, Jouyban-Acree and Jouyban-Acree-Van't Hoff" models with root mean square deviations of < 2.0%. The maximum and minimum
value of PPN was found in pure THP (9.10 × 10
at
= 318.2 K) and pure water (1.03 × 10
at
= 298.2 K), respectively. In addition, HSP of PPN was observed more closed with that of pure THP. The thermodynamic parameters of PPN were obtained using the activity coefficient model. The results showed an endothermic dissolution of PPN at
= 0.6-1.0 in comparison to other THP + water combinations studied. In addition, PPN dissolution was recorded as entropy-driven at
= 0.8-1.0 compared with other THP + water mixtures evaluated.
is an important source of gum Arabic. The availability, traditional, medicinal, pharmaceutical, nutritional, and cosmetic applications of gum acacia have pronounced its high economic value and ...attracted global attention. In addition to summarizing the inventions/patents applications related to gum
, the present review highlights recent updates regarding its phytoconstituents. Traditional, cosmetic, pharmaceutical, and medicinal uses with the possible mechanism of actions have been also reviewed. The patent search revealed the identification of 30 patents/patent applications of
. The first patent related to
was published in 1892, which was related to its use in the prophylaxis/treatment of kidney and bladder affections. The use of
to treat cancer and osteoporosis has also been patented. Some inventions provided compositions and formulations containing
or its ingredients for pharmaceutical and medical applications. The inventions related to agricultural applications, food industry, cosmetics, quality control of gum Arabic, and isolation of some chemical constituents (L-rhamnose and arabinose) from
have also been summarized. The identification of only 30 patents/patent applications from 1892 to 15 November 2021 indicates a steadily growing interest and encourages developing more inventions related to
. The authors recommend exploring these opportunities for the benefit of society.
The current research work was performed to evaluate the solubilization behavior, solution thermodynamics, and solvation behavior of poorly soluble pyridazinone derivative i.e., 6-phenyl-pyridazin-3(2
...)-one (PPD) in various binary solvent systems of dimethyl sulfoxide (DMSO) and water using experimental and various computational approaches. The solubility of PPD in various binary solvent system of DMSO and water was investigated within the temperature range
= 298.2 K to 318.2 K at constant air pressure
= 0.1 MPa, by employing an isothermal technique. The generated solubility data of PPD was computationally represented by five different cosolvency models including van't Hoff, Apelblat, Yalkowsky-Roseman, Jouyban-Acree, and Jouyban-Acree-van't Hoff models. The performance of each computational model for correlation studies was illustrated using root mean square deviations (
). The overall
value was obtained <2.0% for each computational model. The maximum solubility of PPD in mole fraction was recorded in neat DMSO (4.67 × 10
at
= 318.2 K), whereas the lowest one was obtained in neat water (5.82 × 10
at
= 298.2 K). The experimental solubility of PPD in mole fraction in neat DMSO was much higher than its ideal solubility, indicating the potential of DMSO for solubility enhancement of PPD. The computed values of activity coefficients showed maximum molecular interaction in PPD-DMSO compared with PPD-water. Thermodynamic evaluation showed an endothermic and entropy-driven dissolution of PPD in all the mixtures of DMSO and water. Additionally, enthalpy-entropy compensation evaluation indicated an enthalpy-driven mechanism as a driven mechanism for the solvation property of PPD.
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