Polydispersity Index Values Research Articles

Formulation and in vitro evaluation of meloxicam as a self-microemulsifying drug delivery system.

Background: The nonsteroidal anti-inflammatory medication meloxicam (MLX) belongs to the oxicam family and is used to reduce inflammation and pain. The aim of this study was to improve MLX's dispersibility and stability by producing it as a liquid self-microemulsifying drug delivery system since it is practically insoluble in water. Methods: Five different formulations were made by adjusting the amounts of propylene glycol, Transcutol P, Tween 80, and oleic acid oil and establishing a pseudo-ternary diagram in ratios of 1:1, 1:2, 1:3, 1:4, and 3:4, respectively. All of the prepared formulations were tested for a variety of properties, including thermodynamicstability, polydispersity index, particle size distributions, dilution resistance, drug contents, dispersibility, in vitro solubility of the drug, and emulsification time. Results: F5 was chosen as the optimal MLX liquid self-microemulsion due to its higher drug content (99.8%), greater in vitro release (100% at 40 min), smaller droplet size (63 nm), lower polydispersity index (PDI) value (0.3), and higher stability (a zeta potential of -81 mV). Conclusions: According to the data provided here, the self-microemulsifying drug delivery system is the most practical method for improving the dispersibility and stability of MLX.

Erlotinib-Loaded Dendrimer Nanocomposites as a Targeted Lung Cancer Chemotherapy.

Lung cancer is the main cause of cancer-related mortality globally. Erlotinib is a tyrosine kinase inhibitor, affecting both cancerous cell proliferation and survival. The emergence of oncological nanotechnology has provided a novel drug delivery system for erlotinib. The aims of this current investigation were to formulate two different polyamidoamine (PAMAM) dendrimer generations-generation 4 (G4) and generation 5 (G5) PAMAM dendrimer-to study the impact of two different PAMAM dendrimer formulations on entrapment by drug loading and encapsulation efficiency tests; to assess various characterizations, including particle size distribution, polydispersity index, and zeta potential; and to evaluate in vitro drug release along with assessing in situ human lung adenocarcinoma cell culture. The results showed that the average particle size of G4 and G5 nanocomposites were 200 nm and 224.8 nm, with polydispersity index values of 0.05 and 0.300, zeta potential values of 11.54 and 4.26 mV of G4 and G5 PAMAM dendrimer, respectively. Comparative in situ study showed that cationic G4 erlotinib-loaded dendrimer was more selective and had higher antiproliferation activity against A549 lung cells compared to neutral G5 erlotinib-loaded dendrimers and erlotinib alone. These conclusions highlight the potential effect of cationic G4 dendrimer as a targeting-sustained-release carrier for erlotinib.

Formulation and Biomedical Activity of Oil-in-Water Nanoemulsion Combining Tinospora smilacina Water Extract and Calophyllum inophyllum Seeds Oil.

Tinospora smilacina is a native plant used in traditional medicine by First Nations peoples in Australia to treat inflammation. In our previous study, an optimised Calophyllum inophyllum seed oil (CSO) nanoemulsion (NE) showed improved biomedical activities such as antimicrobial, antioxidant activity, cell viability and in vitro wound healing efficacy compared to CSO. In this study, a stable NE formulation combining T. smilacina water extract (TSWE) and CSO in a nanoemulsion (CTNE) was prepared to integrate the bioactive compounds in both native plants and improve wound healing efficacy. D-optimal mixture design was used to optimise the physicochemical characteristics of the CTNE, including droplet size and polydispersity index (PDI). Cell viability and in vitro wound healing studies were done in the presence of CTNE, TSWE and CSO against a clone of baby hamster kidney fibroblasts (BHK-21 cell clone BSR-T7/5). The optimised CTNE had a 24 ± 5 nm particle size and 0.21± 0.02 PDI value and was stable after four weeks each at 4 °C and room temperature. According to the results, incorporating TSWE into CTNE improved its antioxidant activity, cell viability, and ability to promote wound healing. The study also revealed that TSWE has >6% higher antioxidant activity than CSO. While CTNE did not significantly impact mammalian cell viability, it exhibited wound-healing properties in the BSR cell line during in vitro testing. These findings suggest that adding TSWE may enhance CTNE's potential as a wound-healing treatment. This is the first study demonstrating NE formulation in which two different plant extracts were used in the aqueous and oil phases with improved biomedical activities.

Characterization of Spanlastic System Loaded Green Tea Extract as Antioxidant for Skin

Background: Green tea possesses abundant polyphenols that exert antioxidant activity. However, green tea’s hydrophilicity and instability limit its penetration into the skin layers. Recently, a non-ionic surfactant-based elastic nanovesicular system called spanlastic can enhance the delivery of hydrophilic and unstable substances. Spanlastic composed of vesicle builder and edge activator, which influence the characteristics of the vesicle. Objective: The study aimed to evaluate the influence of the ratio of the components on the characterization of green tea extract-loaded spanlastic using three different weight ratio of vesicle builder and edge activator that is 7:3, 8:2, and 9:1. Methods: Spanlastic is prepared by ethanol injection methods using Span 60 as vesicle builder (VB) and Tween® 60 as edge activator (EA). The characterization includes visually observed organoleptic, particle size (PS) and polydispersity index (PDI) using dynamic light scattering, entrapment efficiency (EE) and drug loading (DL) using total phenolic content assay. The most optimum ratio will be tested its zeta potential value using Zetasizer and viscosity using Brookfield Cone and Plate. Results: Selected spanlastic formula composed of Span 60 and Tween® 60 at a weight ratio of 8:2 has given characteristics as follows: entrapment efficiency 60.85±1.70%; drug loading 11.07±0.65%; the particle size is 419.70±7.42 nm; and PDI value 0.26±0.05. The prepared spanlastic has a greenish liquid form, with a zeta potential value of 28.53±2.78 mV and viscosity of 14.65±0.32 cP. Conclusion: The optimum weight ratio of vesicle builder and edge activator for green tea extract spanlastic is Span 60:Tween® 60 8:2.

Effect of Different Lipid Ratios on Physicochemical Stability and Drug Release of Nanostructured Lipid Carriers Loaded Coenzyme Q10

Background: For treatment or skin care via topical route, Coenzyme Q10 needs to permeate the epidermis which it is practically insoluble in water and a high molecular weight that make it difficult to penetrate the skin. Nanostructured Lipid Carriers (NLC) is chosen because of its ability to dissolve and solve the problem of low skin permeation. The type and ratio of solid and liquid lipids used in NLC affect the physicochemical characteristics, thus affecting the release profile and system stability. Objective: This study aimed to determine the effect of various ratios of Compritol 888 ATO as solid lipid and Miglyol 812 as liquid lipid on the physicochemical stability and Coenzyme Q10 release profile of NLC system. Methods: NLC was prepared using High Shear Homogenization method with three different lipid ratios. The ratio of Compritol 888 ATO : Miglyol 812 was 70:30, 80:20, and 90:10, respectively. NLC was evaluated for drug release and stability parameters including organoleptic, particle size, polydispersity index (PI), pH, viscosity, assay, and entrapment efficiency. Results: The stability test result for 90 days showed increments in the particle size and viscosity, whereas for assay and entrapment efficiency were decreased. The release test results showed no significant difference in the release parameters of the three tested formulas. Conclusion: During stability evaluation, NLC-CoQ10 systems did not significantly change pH and PI values, but statistically significantly changed particle size, viscosity, assay, and entrapment efficiency. The different in lipid ratios used in the formulas did not show significantly different results for release parameters.

Factorial Design for the Optimization of Clindamycin HCl-Loaded Ethosome with various concentrations of Phospholipon 90g and Ethanol

Clindamycin HCl is a drug for the treatment of acne. Clindamycin can act as an anti-acne by interfering with bacterial protein synthesis. The concentration of clindamycin used in the treatment of acne is 1%. Still, the bioavailability of the drug in the serum only reaches 0.7 – 12.4% of the total active substance in the preparation, so it is necessary to develop preparations that can increase the bioavailability of the drug Clindamycin HCl, one of which is in the form of ethosomes. This study aimed to optimize the clindamycin HCl loaded ethosomes formula with variations in the concentration of Phospholipon 90G and ethanol using the 22 factorial design method to obtain four formulas. The concentrations of phospholipon 90G used were 2% and 4%, while ethanol was 20% and 40%, respectively. Ethosomes were prepared using the thin layer hydration method and characterized by percent entrapment efficiency (%EE), particle size, and polydispersity index to determine the optimum formula. Based on the factorial design analysis results, the concentration of Phosholipon 90G, ethanol, and their two interactions significantly affected the value of entrapment efficiency, particle size, and polydispersity index with p<0.05. The optimum formula was obtained using 2% phospolipon 90G and 40% ethanol with an entrapment efficiency of 98.31±0.06, a particle size of 179.6±8.6nm, and a polydispersity index of 0.361±0.015. The optimum formula also showed good solubility in distilled water and acid solvents and good physical stability.

Lyophilized nano-liposomal system for red onion (Allium cepa L.) peel anthocyanin: Characterization, bioaccessibility and release kinetics

In recent years, there has been extensive research on valorization of food wastes and a growing interest in nano-liposomal systems for food applications. This paper discusses the case of phosphatidylcholine basednanophytosomes loaded with anthocyanins extracted from red onion (RNPs) to overcome the bio-stability during digestion. The characterization of lyophilized RNPs in terms of entrapment efficiency, particle size, poly-dispersity index (PDI), ζ-potential, morphological properties, in vitro bioaccessibility and release kinetics were investigated. Entrapment efficiency was determined as 78.63% with lowest particle size (177.73 nm) and PDI value (0.45) and non-dense spherical microstructure for RNP6 (red onion peel anthocyanin extract: soybean phosphatidylcholine at 1:6 ratio). Apart from the particle size, entrapment efficiency was determined higher than 75%, which indicates good entrapment. Additionally, from the cumulative release of RNPs concluded as a successful nano-structure with a two-fold increase in intestinal medium. However, poor Carr index and Hausner ratio suggest some limitations of the current nanoliposomes process which could be further improved. Red onion peel wastes, which are typically discarded, can serve as excellent sources of anthocyanins, and its preparation to nanophytosomes could be used as functional food ingredient or food supplements.

Rheology and stability of drilling fluids formulated with saturated NaCl and CaCl2 solutions

Drilling fluids continue under development, being a challenge for the oil industry, which attempts to optimize technical performance, to comply with environmental laws, and to reduce fluid costs. A non-aqueous based drilling fluid widely used by Petrobras has been reformulated due to changes in Brazilian environmental legislation. The paraffinic base of the drilling fluid was replaced by an olefinic base, which is more biodegradable. Hence, to improve drilling fluid performance, the characteristics of olefin emulsions formulated with saturated NaCl and CaCl2 solutions were investigated. Therefore, for different emulsifier concentrations and stirring speeds, the droplet size distribution, the stability, and the rheological parameters of three emulsions were evaluated. All these emulsions had distinct dispersed phases, being these saturated solutions of NaCl, CaCl2, and 75% NaCl and 25% CaCl2. The increase of the stirring speed was followed by the emulsified systems apparent viscosities increase, but their polydispersity index and D50 values were reduced. The NaCl/Olefin emulsion exhibited lower stability, apparent viscosity, and emulsifier saturation concentration when compared to the CaCl2/Olefin emulsion. Besides, the CaCl2/Olefin emulsion showed more pronounced thixotropic behaviour.

Astaxanthin encapsulation in nanocapsule by high-pressure homogenization technology: a study on stability, antioxidant activity and in vitro release

The astaxanthin nanocapsules (ASX-LNC) was prepared by high-pressure homogenization technology, the microstructure, stability, antioxidant activity, and in vitro release characteristics of ASX-LNC were characterized and evaluated. The ASX-LNC comprised a core material and wall materials. The core material was composed of astaxanthin oil, and the wall materials were composed of β-cyclodextrin, decapolyglycerol monooleate, soybean lecithin (PC60), glycerol, and deionized water. The mean particle size of the ASX-LNC was 206.9 ± 2.8 nm, and the polydispersity index (PdI) value was 0.218 ± 0.026. The zeta potential of ASX-LNC was −26.16 ± 0.87 mV. The loading amount of ASX-LNC was 0.546%±0.032%, and the encapsulation efficiency was 99.65%±0.13%, indicating that the preparation process was feasible. The stability of ASX-LNC was determined under different conditions, indicating good stability of the ASX-LNC. In antioxidant research, the inhibition rate of free radicals of ASX-LNC was 91.03 ± 0.87% under 250 μg/mL for 30 min, and the inhibition rate of free radicals of astaxanthin ethanol solution was 90.83 ± 1.37%. The antioxidant capacity of astaxanthin was not affected by the encapsulation, which demonstrated the effect of prolonging the release of active ingredients due to the protection of the biological activity of astaxanthin by encapsulation. Compared with the astaxanthin ethanol solution, the ASX-LNC had a slow-release effect and could prolong the action time of active substances. Overall, ASX-LNC is a potential carrier for application in food and health products, which can control the release of active substances.

Enhanced biopharmaceutical performance of brick dust molecule nilotinib via stabilized amorphous nanosuspension using a facile acid-base neutralization approach.

"Brick dust" compounds have high lattice energy as manifested by the poor aqueous solubility and suboptimal bioavailability. Nilotinib being a weakly basic brick dust molecule exhibits erratic and limited absorption during gastrointestinal transit, attributed to pre-absorptive factors like pH-dependent solubility, poor dissolution kinetics, and post-absorptive factors including P-gp-mediated drug efflux. In our study, these problems are addressed holistically by the successful fabrication of amorphous nanosuspension by an acid-base neutralization approach. The nanosuspension was obtained via rapid precipitation of nilotinib in an amorphous form and the generated in situ sodium chloride salt assisted in stabilizing the drug-loaded nanosuspension in a cage of salt and micellar stabilizer. Soluplus® and hypromellose acetate succinate (HPMCAS) were employed as a novel combination of stabilizers. Systematic optimization was carried out by employing the I-optimal method using Design Expert®software with a concentration of HPMCAS and Soluplus®as independent variables and evaluating them for responses viz particle size, polydispersity index (PDI), and zeta potential. The resultant nanosuspension showed a mean particle size of 130.5 ± 1.22nm with a PDI value of 0.27 ± 0.01, and a zeta potential of - 5.21 ± 0.91mV. The nanosuspension was further characterized for morphology, dissolution, and in vivo pharmacokinetics study. X-ray powder diffraction study of the nano-formulation displayed a halo pattern revealing the amorphous form. Stability studies showed that the nanosuspension remained stable at 40°C ± 2°C and 75% RH ± 5% RH for a period of three months. In vitro drug release and solubility study showed threefold and 36-fold enhancement in dissolution and solubility of the nanosuspension. Furthermore, an in vivo pharmacokinetic study in Sprague-Dawley rats following oral administration displayed a 1.46-fold enhancement in the relative bioavailability of the nanosuspension in contrast to neat nilotinib.

Preparation and characterization of dextran-zein-curcumin nanoconjugate for enhancement of curcumin bioactivity

Curcumin is one of the most important polyphenolic nutrients in pharmaceutical industries. Unfortunately, its poor solubility and bioavailability have hampered its clinical application. To improve curcumin solubility and bioavailability, a natural nanocarrier made from protein-polysaccharide conjugate has been developed. Following antisolvent precipitation method, zein (Z) nanoparticles coated with dextran sulphate (DS) have been fabricated as curcumin (C) nanocarrier (DSZCNPs). The physicochemical properties of the nanoconjugate were measured using different techniques. Morphologically, DSZCNPs appeared spherical and monodispersed in scanning electron microscope (SEM) and transmission electron microscope (TEM) images. Curcumin encapsulation efficiency was ≈ 96%. DSZCNPs size was 180 nm and the polydispersity index value (PDI) 0.28. Zeta potential for DSZCNPs was −28.5 mV. DSZCNPs showed stability either for shelf storage (100 days) or at different pHs. Furthermore, DSZCNPs protected zein nanoparticles degradation in gastric environment and achieved controlled curcumin release in intestinal environment. DSZCNPs greatly enhanced the antioxidant activity of curcumin as demonstrated by DPPH assay. DSZCNPs had significant results in the reduction of colony forming unit (CFU%) against the tested microbes when compared with free curcumin. Also, the anticancer activity of DSZCNPs and free curcumin against hepatocellular carcinoma cells (HepG2) were assessed by MTT assay. IC50 for DSZCNPs was 13 µg/ml compared to 50 µg/ml for free curcumin indicating the therapeutic impact of DSZCNPs over free curcumin. Based on the above results, the developed zein-dextran nanocomplex exhibited high stability and improved the efficacy and bioactivity of curcumin suggesting its potential utility as nanovehicle for the hydrophobic drug curcumin.

Formulation and Evaluation of Tea tree/ Rosemary Essential oil-based Microemulsion for Antimicrobial Activity

ABSTRACT: This research aims to prepare microemulsion from Tea Tree and Rosemary essential oil to treat gram-positive and gram-negative bacterial infections. A phase titration has been used to make the proposed microemulsion, which contained 71% water, 23% of a 1:1 mixture of propylene glycol (surfactant), tween 80 (co-surfactant), and 6% of tea tree/rosemary essential oil. In Rosemary essential oil pale yellowish transparent microemulsion, droplet size, zeta potential, and polydispersity index (PDI) of 58.9, 883.6, and 0.678, respectively, showed a stable microemulsion. Tea tree oil loaded in a light, clear microemulsion with zeta potential, droplet size, and polydispersity index (PDI) values of 265.9, 746.8, and 0.987, respectively, indicated a stable microemulsion. The RMO/TTO micro emulsion's viscosity was 1.844/1.933 cps, and its pH ranged from 4.69 to 5.59. The formulation was determined to be a safe, reliable, and effective one in light and good in stability experiments. Escherichia coli, Staphylococcus aureus, and Candida albicans can all be treated using a microemulsion that contains 6% tea tree oil and rosemary oil by agar well diffusion method. Both the EOs-based microemulsion showed more zone of inhibition against Escherichia coli and Candida albicans while Staphylococcus aureus is the less susceptible zone of inhibition. The microemulsion formulation's minimum inhibitory concentration was effective against Staphylococcus aureus, Candida albicans, and E. coli on all physiological parameters. It can be concluded that TTO/RMO essential oil-loaded microemulsion is considered a promising substitute for the current gram-positive and gram-negative regimens.

Binary ethosomes for the enhanced topical delivery and antifungal efficacy of ketoconazole

This work aimed to prepare ketoconazole-loaded ethosomes and binary ethosomes to improve its skin delivery and antifungal efficacy. A 32 factorial design was used to optimize the ethosomes and formulate ketoconazole-loaded binary ethosomes. Ethosomes and binary ethosomes were evaluated for particle size, polydispersity index, zeta potential, percent drug entrapment efficiency, drug release, skin permeation and deposition and antifungal efficacy. The ethosomes particle size ranged from 78.99±16.72 to 321.53±10.41 nm and decreased by increasing phospholipid and ethanol concentrations. The polydispersity index values were in the range of 0.17±0.01 to 0.49 ± 0.04. The percent drug entrapment efficiency ranged from 36.09±2.66 to 95.89±0.19 and increased by increasing phospholipid concentration while ethanol concentration had the opposite effect. The binary ethosomes had smaller size but similar drug entrapment efficiency and zeta potential compared with the ethosomes. They had significantly higher percent drug release (∼96%) and permeation (∼95%) through rat skin compared with the ethosomes (93% and 90%, respectively). Binary ethosomes and ethosomes had, respectively 1.9 and 1.8-fold higher drug skin permeation and 5.3- and 5.6-fold higher drug deposition in the epidermis/dermis compared with the drug suspension. The antifungal efficacy of the drug-loaded ethosomes and binary ethosomes were similar to the drug hydroalcoholic solution. Collectively, these results confirm the potential of these nanocarriers to enhance drug efficacy given their small size, sustained drug release and enhanced skin permeability.

Formulation and in vitro evaluation of meloxicam as a self-microemulsifying drug delivery system

Background: The nonsteroidal anti-inflammatory medication meloxicam (MLX) belongs to the oxicam family and is used to reduce inflammation and pain. The aim of this study was to improve MLX's dispersibility and stability by producing it as a liquid self-microemulsifying drug delivery system since it is practically insoluble in water. Methods: Five different formulations were made by adjusting the amounts of propylene glycol, Transcutol P, Tween 80, and oleic acid oil and establishing a pseudo-ternary diagram in ratios of 1:1, 1:2, 1:3, 1:4, and 3:4, respectively. All of the prepared formulations were tested for a variety of properties, including thermodynamic stability, polydispersity index, particle size distributions, dilution resistance, drug contents, dispersibility, in vitro solubility of the drug, and emulsification time. Results: F5 was chosen as the optimal MLX liquid self-microemulsion due to its higher drug content (99.8%), greater in vitro release (100% at 40 min), smaller droplet size (63 nm), lower polydispersity index (PDI) value (0.3), and higher stability (a zeta potential of -81 mV). Conclusions: According to the data provided here, the self-microemulsifying drug delivery system is the most practical method for improving the dispersibility and stability of MLX.

Synthesis of Sulfonated Polyphenylene Block Copolymers via In Situ Generation of Ni(0)

Proton exchange membranes (PEMs) fabricated from sulfonated polyphenylenes (sPP) exhibit superior proton conductivity and electrochemical performance. However, the Ni(0) catalyst required for Colon's cross-coupling reaction for the synthesis of sPP block copolymers is expensive. Therefore, in this study, we generated Ni(0) in situ from an inexpensive Ni(II) salt in the presence of the reducing metal Zn and NaI. The sPP block copolymers were synthesized from neopentyl-protected 3,5- and 2,5-dichlorobenzenesulfonates and oligo(arylene ether ketone) using the catalyst NiBr2(PPh3)2. The block copolymers synthesized using our strategy and the Ni(0) catalyst exhibited comparable polydispersity index values and high molecular weights. Thin, transparent, and bendable PEMs fabricated using selected high-molecular-weight sPP block copolymers synthesized via our strategy exhibited similar proton conductivities to those of the block copolymers synthesized using the Ni(0) catalyst. We believe that our strategy will promote the synthesis of similar multifunctional block copolymers.

Development and characterization of clove oil microemulsion

Clove oil is one type of essential oil from clove flower buds (Syzygium aromaticum) which contains eugenol compounds. Clove oil is volatile in nature and highly affected by heat, thus incorporating it in a microemulsion system can increase its shelf life of the oils. This study aimed to formulate and characterize microemulsion preparations with clove flower essential oil. The microemulsion existence region was determined by constructing a pseudo-ternary phase diagrams and prepared with four components, i.e. isopropyl myristate, tween-80 as a surfactant, polyethylene glycol 400 (PEG 400) as a co-surfactant, and water as the aqueous phase. The optimized clove oil microemulsion formulation was subjected to an evaluation of various parameters, such as organoleptic properties, %transmittance, pH, viscosity, stability, particle size, zeta potential, and polydispersity index (IP). Based on the results of the study, the highest compound component in clove oil was eugenol with a % area of ​​63.79%. The results revealed that the construction of a phase diagram and the use of the phase titration method constituted a suitable technique for the preparation of microemulsions as most of the formulations were transparent. It was found that the tween-80:PEG 400 ratio of 2:1 with an oil:S-mix ratio of 1:9 generated an optimum results. The clove oil microemulsion had a globule size of 17.69±0.025nm, a polydispersity index value of 0.057±0.0043, zeta potential of-5.36±0.23mV, and a pH value of 7.3±0.1, a viscosity value of 466.7±9.06., and %transmittance of 99.9±0.1. According to these findings, the microemulsion formulation might serve as a suitable drug delivery system.

PH-Responsive Poly(ethylene glycol)-b-poly(2-vinylpyridine) Micelles for the Triggered Release of Therapeutics

The use of pH-responsive polymeric micelles is a promising approach to afford the targeted, pH-mediated delivery of hydrophobic drugs within the low-pH tumour milieu and intracellular organelles of cancer cells. However, even for a common pH-responsive polymeric micelle system-e.g., those utilising poly(ethylene glycol)-b-poly(2-vinylpyridine) (PEG-b-PVP) diblock copolymers-there is a lack of available data describing the compatibility of hydrophobic drugs, as well as the relationships between copolymer microstructure and drug compatibility. Furthermore, synthesis of the constituent pH-responsive copolymers generally requires complex temperature control or degassing procedures that limit their accessibility. Herein we report the facile synthesis of a series of diblock copolymers via visible-light-mediated photocontrolled reversible addition-fragmentation chain-transfer polymerisation, with a constant PEG block length (90 repeat units (RUs)) and varying PVP block lengths (46-235 RUs). All copolymers exhibited narrow dispersity values (Đ ≤ 1.23) and formed polymeric micelles with low polydispersity index (PDI) values (typically <0.20) at physiological pH (7.4), within a suitable size range for passive tumour targeting (<130 nm). The encapsulation and release of three hydrophobic drugs (cyclin-dependent kinase inhibitor (CDKI)-73, gossypol, and doxorubicin) were investigated in vitro at pH 7.4-4.5 to simulate drug release within the tumour milieu and cancer cell endosome. Marked differences in drug encapsulation and release were observed when the PVP block length was increased from 86 to 235 RUs. With a PVP block length of 235 RUs, the micelles exhibited differing encapsulation and release properties for each drug. Minimal release was observed for doxorubicin (10%, pH 4.5) and CDKI-73 exhibited moderate release (77%, pH 4.5), whereas gossypol exhibited the best combination of encapsulation efficiency (83%) and release (91% pH 4.5) overall. These data demonstrate the drug selectivity of the PVP core, where both the block molecular weight and hydrophobicity of the core (and accordingly the hydrophobicity of the drug) have a significant effect on drug encapsulation and release. These systems remain a promising means of achieving targeted, pH-responsive drug delivery-albeit for select, compatible hydrophobic drugs-which warrants their further investigation to develop and evaluate clinically relevant micelle systems.

Antioxidant and hypoglycemic potential of phytogenic cerium oxide nanoparticles

Plants provide humans with more than just food and shelter; they are also a major source of medications. The purpose of this research was to investigate the antioxidant and hypoglycemic potential of green synthesized CeONPs using Mentha royleana leaves extract. The morphological and physicochemical features of CeONPs were evaluated by UV–Visible spectrophotometry, Scanning Electron Microscopy, Energy Dispersive X-rays and Fourier-transform infrared spectrometry, Dynamic light scattering, Atomic Force Microscopy, Zeta Potential. The average size range of synthesized CeONPs diameter between 46 and 56 nm, crystalline in shape, with Polydispersity index value of 0.2 and subatomic particles mean diameter was 4.5–9.1 nm. The antioxidant capability of CeONPs was assessed using DPPH, ABTS+, hydrogen peroxide, hydroxyl radical scavenging, and reducing power tests. The hypoglycemic potential of CeONPs was investigated using alpha-amylase, alpha-glucosidase, glucose absorption by yeast cells, and antisucrase. The effective concentrations were 500 and 1000 µg/ml found good in suppressing radical species. To explore the hypoglycemic potential of CeONPs, alpha-amylase, alpha-glucosidase, glucose absorption by yeast cell, and antisucrase assays were performed. Glucose absorb by yeast cells assay was tested for three distinct glucose concentrations: 5 mmol/L, 10 mmol/L, and 25 mmol/L. Green synthesize CeONPs showed a dose-dependent response, higher concentrations of CeONPs imposed a stronger inhibitory impact on the catalytic site of enzymes. This study suggest that CeONPs could possibly binds to the charge carrying species and act as competitive inhibitor which slow down the enzyme substrate reaction and prevents enzymatic degradation. The study’s findings were outstanding, which bodes well for future medicinal applications of CeONPs.

Enhanced Bioactivity of Rosemary, Sage, Lavender, and Chamomile Essential Oils by Fractionation, Combination, and Emulsification.

This study aimed to increase the bioactivity of essential oils by fractionation, combination, and emulsification. In this regard, pharmaceutical quality Rosmarinus officinalis L. (rosemary), Salvia sclarea L. (clary sage), Lavandula latifolia Medik. (spike lavender), and Matricaria chamomilla L. (chamomile) essential oils were fractionated by vacuum-column chromatography. The main components of the essential oils were verified, and their fractions were characterized by thin layer chromatography, gas chromatography-flame ionization detector, and gas chromatography/mass spectrometry. Besides, oil-in-water (O/W) emulsions of essential oils and diethyl ether fractions were obtained by the self-emulsification method, followed by droplet size, polydispersity index, and zeta potential value measurements. The in vitro antibacterial effects of the emulsions and binary combinations (10:90, 20:80, 30:70, 40:60, 50:50, 60:40, 70:30, 80:20, 90:10, v:v) against Staphylococcus aureus were determined by microdilution. In addition, the in vitro anti-biofilm, antioxidant, and anti-inflammatory effects of emulsion formulations were evaluated. According to the experimental results, fractionation and emulsification enhanced essential oil in vitro antibacterial, anti-inflammatory, and antioxidant effects due to increased solubility and nano-sized droplets. Among 22 different emulsion combinations, 1584 test concentrations resulted in 21 cases of synergistic effects. The mechanism of the increase in biological activities was hypothesized to be higher solubility and stability of the essential oil fractions. Food and pharmaceutical industries may benefit from the procedure proposed in this study.

Enhanced Antibacterial Activity of Piper betle Extract Niosome Serum Gel and Its Irritation Effects

Masks are personal protective equipment essential for COVID-19 prevention, but for the use of masks has led to an increase in the severity of both acne (maskne) and rosacea (mask rosacea). Long-time mask-wearing can increase acne’s flare by modifying the cutaneous facial microenvironment and triggering facial dermatoses. To minimize this, the skin needs to be protected by using an antibacterial product. This study aimed to develop and determine the antibacterial effect of Piper betle extract in niosome serum gel and its irritation effect. 5% Piper betle extract was formulated into a niosome system and incorporated into the serum gel with varying concentrations of 30%, 40%, and 50%. The niosome system was characterized by particle size, Polydispersity Index (PI), zeta potential, and pH value, and then evaluated physicochemical properties for niosome serum gel preparation. Further, the antibacterial effect against Propionibacterium acne, Staphylococcus aureus, and Staphylococcus epidermidis was tested using a well-diffusion test. The preparation stability was evaluated using freeze-thaw methods, and the irritation test was assessed using the HET-CAM (Hen’s Egg Chorioallantoic Membrane) method. The results showed that the preparation has a good physicochemical, while the best inhibition zone diameter was 7,29±0,21; 7,77±0,12; and 8,24±0,40, against P.acne, respectively. However, the results of the stability test of the preparation showed a significant change in the pH but had no irritation effect on CAM. It can concluded that the niosome serum gel of Piper betle extract has a potential antibacterial impact for acne, especially against P. acne.&#x0D; Keywords: Piper betle, Niosome serum gel, antibacterial effect, stability, irritation effect