High Entrapment Efficiency Research Articles

Natural Stabilizers and Nanostructured Lipid Carrier Entrapment for Photosensitive Compounds, Curcumin and Capsaicin.

Capsaicin and curcumin, the active components of chili and turmeric, are prone to instability when exposed to light. Therefore, this research aimed to enhance the photostability of both extracts via the use of antioxidants, natural sunscreen, and nanostructured lipid carriers (NLCs). NLCs were chosen for this this study due to their advantages in terms of stability, drug loading capacity, occlusive effect, skin penetration, and controlled release. The photostability of each extract and extracts mixed with antioxidants, including grape seed extract, tea extract, and chlorogenic acid, were determined. Chlorogenic acid can enhance the photostability of capsaicin from 6.79 h to 16.50 h, while the photostability of curcumin increased from 9.63 h to 19.25 h. In addition, the use of natural sunscreen (sunflower oil) also increased the photostability of capsaicin and curcumin. The mixed extracts were then loaded into NLCs. The particle size of the formulation was 153.73 nm with a PDI value of 0.25. It exhibited high entrapment efficiency (more than 95%). In addition, it effectively reduced the decomposition of capsaicin and curcumin. Importantly, the natural stabilizers chosen for NLC fabrication significantly improved the photostability of curcumin and capsaicin by 600% and 567% compared to the unstabilized counterparts. This improvement contributes to the sustainability and bioavailability of these compounds in both cosmeceutical and pharmaceutical products.

Fabrication and evaluation of cross-linked nanogels of Dexibuprofen

The objective of this study was to design and develop an Agarose-based polymeric nanogel network system for solubility enhancement of a lipophilic drug, Dexibuprofen. Polymeric nanogels were synthesized through free radical polymerization where Agarose was cross-linked with 2-Acrylamido-2-methylpropane sulfonic acid (AMPS) in the presence of ammonium persulfate (APS) as an initiator and N, N’-Methylenebisacrylamide (MBA) as crosslinking agent. The resulting polymeric nanogels underwent a comprehensive characterization process including Fourier transform infrared (FTIR), particle size analysis, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermal gravimetric analysis (TGA), powder X-ray diffraction (PXRD), and swelling studies to confirm the preparation of a stable polymeric nanogel system. FTIR spectral findings revealed that Agarose was chemically cross-linked with AMPS and confirmed the successful insertion of AMPS chains on the Agarose backbone. Particle size analysis revealed a diameter of 168 nm with a zeta potential of −9.91 mV, providing assurance of a stable polymeric nanogel system. SEM images depicted a highly porous surface. DSC and TGA results showed a more thermally stable network system than individual ingredients. Swelling studies revealed an increased swelling ratio of polymeric nanogels at phosphate buffer of pH 6.8 than acidic buffer of pH 1.2. Dexibuprofen was efficiently loaded into a polymeric nanogel system with a high entrapment efficiency of up to 80%. The solubility of the drug was enhanced when introduced to a polymeric nanogel formulation when compared to pure drug. The system reproducibility was evaluated through in vitro drug release and kinetic modeling of drug release. Toxicity studies confirmed the formulation’s effectiveness, showcasing the developed polymeric nanogels as a promising option for delivering lipophilic drugs, with outstanding physicochemical properties, improved solubility, and minimal oral toxicity.

DESIGN OF JACKFRUIT GUM-BASED GENIPIN CROSSLINKED NANOPARTICLES FOR SUSTAINED RELEASE OF CURCUMIN: OPTIMIZATION AND IN VITRO CHARACTERIZATION

The present work aims to design jackfruit gum-based curcumin-loaded nanoparticles (CUR-NPs) for improved drug entrapment and modified release of CUR using ionotropic gelation. Briefly, the optimization of CUR-NPs was confirmed using a 32 response surface methodology. The diffractogram and thermogram of CUR-NPs confirmed reduction of crystallinity of CUR (optimized batch: F5) due to jackfruit gum and genipin cross-linked polymeric network. The particle size and zeta potential analysis confirmed formation of nanosized and stable CUR-NPs, respectively. Also, the nanoparticles demonstrated 83.99 ± 1.23% entrapment efficiency, whereas they showed 98.36 ± 0.96% of CUR release within 12 h at pH 7.4. The CUR-NPs exhibited good mucoadhesive properties due to the presence of jackfruit gum. Finally, the MTT assay showed a decrease in colorectal cancer cell viability due to tailored CUR release from CUR-NPs. In conclusion, jackfruit gum-genipin-based CUR-NPs offered high entrapment efficiency, tailored releases of CUR, good mucoadhesive property and improved anticancer activity.

Zeolitic Imidazole Framework/Silica Nanocomposite for Targeted Cancer Therapeutics: Comparative Study of Chemo-Drug Cisplatin (CPt) and Green Platinum (GPt) Efficacy.

A chemo-drug such as cisplatin is effective for cancer treatment but remains non-specific, is susceptible to drug resistance, and induces several side effects on organ systems. Zeolitic imidazolate framework-8, a type of MOF, has gained attention, including as a drug delivery method for targeted cancer therapeutics. In this study, ZIF-8/Silica nanocomposite was synthesized using a one-pot hydrothermal technique using the Stober technique. We studied the effect of phyto-synthesized GPt and chemo-drug cisplatin CPt on ZIF-8/Silica for targeted efficacy of cancer therapy. The texture, morphology, and chemical environment of Pt on ZIF-8/Silica were analyzed using different characterization techniques such as XRD, FT-IR, BET, diffuse reflectance spectroscopy, SEM-EDX, TEM, zeta potential, and TGA analysis. The isothermal behavior of CPt and GPt adsorption was investigated using isotherm models like Langmuir, Freundlich, and Temkin isotherm. The adsorption kinetics indicating the adsorption efficiency of GPt and CPt are influenced by the concentration of Pt complex and the adsorption sites of ZIF-8/Silica. A high entrapment efficiency and loading capacity of GPt (86% and 4.3%) and CPt (91% and 4.5%) were evident on ZIF-8/Silica. The nanocomposite showed a pH-sensitive Pt release using a dialysis membrane technique. For instance, a high release of GPt (93%) was observed under pH = 6.6 in 72 h, while the release reduced to 50% at pH 7.4 in 72 h. The anti-cancer activity of nanoformulations was studied in vitro using MCF7 (breast cancer cells) and HFF-1 (human foreskin fibroblast) cells. The findings demonstrated that GPt is as effective as CPt; the EC50 value for MCF7 cells treated with ZIF-8/Silica/Cp/PEG was 94.86 µg/mL, whereas for ZIF-8/Silica/GPt/PEG it was 60.19 µg/mL.

Topical co-delivery of tacrolimus and calcipotriol loaded nanostructured lipid carrier: a potential and synergistic approach in the management of psoriasis

The focus of this study was to develop a Vitamin-D3 (Calcipotriol)-based Tacrolimus (TAC)-loaded nanostructured lipid carrier (NLC) for topical application to treat psoriasis. The sonication technique followed by melt emulsification was used to formulate TAC-NLC, in which Precirol ATO-5, Calcipotriol, and Solutol HS-15 were used as excipients. Based on the analysis of particle size, PDI, and entrapment efficiency of various TAC-NLCs using Box-Behnken Design, an optimized NLC was selected. The selected nanocarrier was further transformed into the gel and then characterized for in vitro release, in vitro and ex vivo permeation, and dermatokinetic, including in vitro characterization studies. The optimized TAC-NLC had a particle size of 231 ± 1.52 nm with a narrow PDI of 0.40 ± 0.001 along with high entrapment efficiency (84.04 ± 1.36%) and drug loading (12.61 ± 0.20%)”. The in vitro release showed sustained release throughout 12 h. Moreover, dissimilarity (f1:52) and the similarity factor (f2:37) showed a lack of any similarity in the evaluation of drug release from TAC-NLC formulation and Conventional formulation. The time requisite to release 50% (T50), 30% (T30), and 20% (T20) of the drug is also calculated. The flux and permeability coefficients were found to be 11.59 µg/cm2/h and 0.0386 cm/h. A dermatokinetic study of TAC-NLC indicated a remarkable rise in AUC0-12h and CSkin max compared to conventional formulation (p < 0.005). Further, the vitro studies indicated higher cell viability (85%-80%) on melanoma cells than aqueous suspension of the drug (60–70%). The study indicated that the topical application of TAC-NLC nanogel was found potentially useful for the management of psoriasis.

Formulation of Lipid Nanoparticles based Nanogel of Sertaconazole Nitrate and its Evaluation

Background: Sertaconazole nitrate is a topical antifungal drug used to treat interdigital tinea pedis in patients with immunocompetent conditions. The class of imidazole includes the antifungal medication sertaconazole nitrate. It is available in topical formulations for treating skin infections, including athlete's foot. Solid lipid nanoparticles (SLN) are at the cutting edge of nanotechnology, with several potential uses in drug delivery and research. Because of their unique size-dependent features, lipid nanoparticles hold the promise of novel therapies. Objective: Drug incorporation into nanocarriers creates a new drug delivery prototype that could be employed for drug targeting. The research aims to study the formulation and evaluation of Sertaconazole nitrate solid lipid nanoparticles. The goal behind formulating SLN gel is to provide and maintain therapeutic concentrations of the drug at the target biological site to maximise therapeutic efficacy and minimise side effects. Methods: Sertaconazole Nitrate Solid Lipid Nanoparticles are prepared by using High Pressure Homogenizer to get nanogel formulation as the final formulation and In-vitro drug release using a diffusion apparatus. The prepared SLNs were evaluated in their FTIR studies to determine compatibility between the drug and the excipients; zeta potential indicates the solid lipid nanoparticle was stable, and polydispersity index was used to determine particle size. Result: The results demonstrate that optimised SLN-based Sertaconazole nitrate gel exhibited the best physicochemical properties, including FTIR studies of the drug, excipients, and optimised formulation demonstrate that all are compatible with each other, particle size is less than 200 nm, zeta potential ranging from 12 to -20 mV, and highest entrapment efficiency is 71.48%. Optimised solid lipid nanoparticles showed good in vitro release and antimicrobial results. The main application of SLN large scale-up is possible, and the drug can be effective with less dose incor-poration. Conclusion: In this research work, the proposed plan of work SLN of Sertaconazole Nitrate was formulated successfully. The preliminary identification tests were performed, such as melting point determination, estimation of λmax by UV-visible spectrophotometry and plot of its calibration curve in solvent and buffer system, and FT-IR investigation to confirm the purity and confirmation of medication. High physical stability and drug loading are advantageous to SLN.

A Nano-Based Approach to Deliver Satureja thymbra Essential Oil to the Skin: Formulation and Characterization.

Essential oils are well known for their biological properties, making them useful for the treatment of various diseases. However, because of their poor stability and high volatility, their potential cannot be fully exploited. The use of nanoformulations to deliver essential oils can solve these critical issues and amplify their biological activities. We characterized an essential oil from Satureja thymbra via GC-MS and HPLC-DAD to provide qualitative and quantitative data. The essential oil was formulated in phospholipid vesicles which were characterized for size, surface charge, and storage stability. The entrapment efficiency was evaluated as the quantification of the major monoterpenoid phenols via HPLC-DAD. The morphological characterization of the vesicles was carried out via cryo-TEM and SAXS analyses. The essential oil's antioxidant potential was assayed via two colorimetric tests (DPPH• and FRAP) and its cytocompatibility was evaluated in HaCaT skin cell cultures. The results showed that the nanoformulations developed for the loading of S. thymbra essential oil were below 100 nm in size, predominantly unilamellar, stable in storage, and had high entrapment efficiencies. The vesicles also displayed antioxidant properties and high cytocompatibility. These promising findings pave the way for further investigation of the therapeutic potential of S. thymbra nanoformulations upon skin application.

MECHANISTIC OUTCOMES OF LIPID CORE ON SOLID LIPID NANOPARTICLE CHARACTERIZATION

In our present study, solid lipid nanoparticles were fabricated by modified double emulsification followed by ultracentrifugation method. The SLNs of the anti-HIV drugs lamivudine, tenofovir disoproxil fumarate and efavirenz were synthesized using lipids Compritol 888 ATO, glyceryl monostearate, stearic acid and emulsifiers soy lecithin and Pluronic®F68. The synthesized SLNs were characterized for compatibility studies, mean particle size, PDI, zeta potential, surface morphology and entrapment studies. The higher amount of Compritol based SLNs formulation showed maximum entrapment efficiency with comparatively larger sized, homogenous particles. All the lipid based SLNs possessed no incompatibilities and showed high stability profiles. Based on the results of surface morphology, zeta potential and high entrapment efficiency values, the optimum lipid for SLNs formulation among the other lipids was determined to be Compritol 888 ATO.

Calcium hydroxide-loaded nanoparticles dispersed in thermosensitive gel as a novel intracanal medicament.

Design, produce and assess the viability of a novel nanotechnological antibacterial thermo-sensible intracanal medicament This involves encapsulating calcium hydroxide (Ca(OH)2) within polylactic-co-glycolic acid (PLGA) nanoparticles (NPs) and dispersing them in a thermosensitive gel (Ca(OH)2-NPs-gel). In addition, perform in vitro and exvivo assessments to evaluate tissue irritation and penetration capacity into dentinal tubules in comparison to free Ca(OH)2. Reproducibility of Ca(OH)₂-NPs was confirmed by obtaining the average size of the NPs, their polydispersity index, zeta potential and entrapment efficiency. Moreover, rheological studies of Ca(OH)2-NPs-gel were carried out with a rheometer, studying the oscillatory stress sweep, the mean viscosity value, frequency and temperature sweeps. Tolerance was assessed using the membrane of an embryonated chicken egg. In vitro Ca(OH)2 release was studied by direct dialysis in an aqueous media monitoring the amount of Ca(OH)2 released. Six extracted human teeth were used to study the depth of penetration of fluorescently labelled Ca(OH)2-NPs-gel into the dentinal tubules and significant differences against free Ca(OH)2 were calculated using one-way anova. Ca(OH)2-NPs-gel demonstrated to be highly reproducible with an average size below 200 nm, a homogeneous NPs population, negative surface charge and high entrapment efficiency. The analysis of the thermosensitive gel allowed us to determine its rheological characteristics, showing that at 10°C gels owned a fluid-like behaviour meanwhile at 37°C they owned an elastic-like behaviour. Ca(OH)2-NPs-gel showed a prolonged drug release and the depth of penetration inside the dentinal tubules increased in the most apical areas. In addition, it was found that this drug did not produce irritation when applied to tissues such as eggs' chorialantoidonic membrane. Calcium hydroxide-loaded PLGA NPs dispersed in a thermosensitive gel may constitute a suitable alternative as an intracanal antibacterial medicament.

Formulating and evaluating a gel that contains Eletriptan-loaded transferosomes

Transdermal-vesicular drug delivery systems offer various advantages over conventional drug delivery systems, such as bypassing first-pass metabolism, site-specific delivery, reduced dosing frequency, and more. The objective of the present research involves the formulation and in-vitro evaluation of Eletriptan transferosomal gel to reduce dosing frequency. Transferosomes act as vehicles for on-site drug delivery, and they are vesicular systems with a flexible membrane. By formulating this type, we can achieve a higher concentration at the site of action, thereby reducing dosing frequency.&#x0D; Fourier-transform infrared spectra revealed that there was no interaction between the drug and excipients. Transferosomal formulations were prepared by the thin-film hydration technique and were incorporated into 1.5% Carbopol gel. From the results, Formulation code-ET6, containing Lecithin: Tween-80, has higher entrapment efficiency and maximum drug release, and is hence considered the optimized formulation. Stability studies performed for optimized transferosomal gel formulations indicate that the prepared transferosomal gel has more stability at a lower temperature.&#x0D; The conclusion is that, based on the above data, it is confirmed that the prepared Eletriptan transferosomal gels can be considered as one of the promising approaches to reducing dosing frequency and maintaining drug concentration at the desired site for a longer time.&#x0D; Keywords: Transdermal drug delivery, Eletriptan, Transferosomes, Thin Film Hydration Method, Carbopol gel.

PH-sensitive docetaxel-loaded chitosan/thiolated hyaluronic acid polymeric nanoparticles for colorectal cancer.

Aim: This study aimed to develop and evaluate pH-sensitive docetaxel-loaded thiolated hyaluronic acid (HA-SH) nanoparticles (NPs) for targeted treatment of colon cancer. Materials & methods: HA-SH, synthesized via oxidation and subsequent covalent linkage to cysteamine, served as the precursor for developing HA-SH NPs through polyelectrolyte complexation involving chitosan and thiol-bearing HA. Results & conclusion: HA-SH NPs displayed favorable characteristics, with small particle sizes (184-270nm), positive zeta potential (15.4-18.6mV) and high entrapment efficiency (91.66-95.02%). In vitro, NPs demonstrated potent mucoadhesion and enhanced cytotoxicity compared with free docetaxel. In vivo assessments confirmed safety and biocompatibility, suggesting HA-SH NPs as promising pH-sensitive drug carriers with enhanced antitumor activity for colorectal cancer treatments.

Evaluation of types and concentration of bile salts impact on physical properties of nisoldipine-loaded bilosomes

Background: Bilosomes are lipid vesicles that exhibit flexibility and deformability. They consist of phospholipids and amphiphilic bile salts. Compared to the normal vesicular systems such as liposomes and niosomes, bilosomes provide several notable advantages, including simplified manufacturing, cost-effectiveness, and enhanced stability. Aim: The main objective of the present work was to evaluate the effect of different bile salts on the physical properties that include entrapment efficiency, vesicle size, and polydispersity index(PDI). In addition, in vitro drug release for nisoldipine (NSD) loaded bilosomes was evaluated. Methods: Nisoldipine-loaded bilosomes were made using a thin film hydration technique. Cholesterol along with surfactant (span 60) was employed, and the formulation also contained several different bile salts, including sodium deoxycholate (SDC), sodium glycocholate (SGC), and sodium taurocholate (STC). Results: The developed NSD bilosomes exhibited an entrapment efficiency ranging from 44.2 ± 0.3 to 82.36 ± 0.80% and a vesicle size diameter in the nanometric dimensions (166 ± 1.83 to 237.8 ± 3.3 nm). An in-vitro release study revealed that formulas prepared with SDC bile salts showed higher drug release than SGC and STC formulas. Increasing the bile salt amount from 5 mg to 10 mg increases entrapment efficiency with increasing vesicle size. Further increase in bile salt led to decreased entrapment efficiency with increased vesicle size. SDC gives the best result in terms of entrapment efficiency and acceptable size. STC provides the largest particle size due to its high molecular weight compared to SGC and SDC. Conclusion: The SDC bile salt component is better suited for manufacturing NSD bilosomes. This is because this component yields the best results regarding high entrapment efficiency, nano size, and prolonged drug release.

Spray-Dried Mucoadhesive Re-dispersible Gargle of Chlorhexidine for Improved Response Against Throat Infection: Formulation Development, In Vitro and In Vivo Evaluation.

Drug delivery to the buccal mucosa is one of the most convenient ways to treat common mouth problems. Here, we propose a spray-dried re-dispersible mucoadhesive controlled release gargle formulation to improve the efficacy of chlorhexidine. The present investigation portrays an approach to get stable and free-flowing spray-dried porous aggregates of chlorhexidine-loaded sodium alginate nanoparticles. The ionic gelation technique aided with the chlorhexidine's positive surface charge-based crosslinking, followed by spray drying of the nanoparticle's dispersion in the presence of lactose- and leucine-yielded nano-aggregates with good flow properties and with a size range of about 120-350nm. Provided with the high entrapment efficiency (87%), the particles showed sustained drug release behaviors over a duration of 10h, where 87% of the released drug got permeated within 12h. The antimicrobial activity of the prepared formulation was tested on S. aureus, provided with a higher zone of growth inhibition than the marketed formulation. Aided with an appropriate mucoadhesive strength, this product exhibited extended retention of nanoparticles in the throat region, as shown by in vivo imaging results. In conclusion, the technology, provided with high drug retention and extended effect, could be a potential candidate for treating several types of throat infections.

Oridonin Loaded Peptide Nanovesicles Alleviate Nonalcoholic Fatty Liver Disease in Mice

This study was to construct a nanovesicle delivery system to improve the loading efficiency and stability of ORI for the treatment of nonalcoholic fatty liver disease (NAFLD). This nanovesicles (NVs) exerted a narrow size distribution (195.6 ± 11.49 nm) and high entrapment efficiency (84.46 ± 1.34%). In vitro cell studies demonstrated that the NVs treatment enhanced the cellular uptake of ORI and reduced lipid over-accumulation and total cholesterol levels in NAFLD cell model. At the same time, in vivo study proved that, compared with the normal group, the model group mice showed a decrease in body weight, a significant increase in liver index (6.71 ± 0.62, p < 0.01), and symptoms of liver lipid accumulation, lipid vesicles, and liver tissue fibrosis. Compared with the model group, after high-dose ORI NVs intervention, mice gained weight, decreased liver index (4.69 ± 0.55, p < 0.01), reduced hepatic lipid droplet vacuoles, reduced lipid accumulation (reduced oil red area, p < 0.001), and alleviated the degree of liver fibrosis (reduced blue collagen area, p < 0.001). In conclusion, ORI/HP-β-CD/H9-HePC NVs showed specific liver accumulation and improved therapeutic effects, the nano drug loading system provides a promising strategy for the encapsulation of ORI to effectively alleviate the process of NAFLD.

Entrapment of Digoxin-KLH Conjugate in Alginate/Chitosan Nanoparticles: A New Antigen Delivery System For Production of Anti-digoxin Antibodies.

Nanoparticles have received more and more attention in the vaccine and drug delivery systems field due to their specific properties. In particular, alginate and chitosan have been known as the most promising nano-carries. Digoxin-specific antibodies effectively manage acute and chronic digitalis poisoning using sheep antiserum. The present study aimed to develop alginate/chitosan nanoparticles as a carrier of Digoxin-KLH to promote the immune response by improving the hyper-immunization of animals. The nanoparticles were produced by the ionic gelation method in mild conditions and the aqueous environment, which leads to the production of particles with favorable size, shape, high entrapment efficiency, and controlled release characteristics. The synthesized nanoparticles of 52 nm in diameter, 0.19 in PDI, and -33mv in zeta potential were considerably unparalleled and characterized by SEM, FTIR, and DSC. Nanoparticles resembled a spherical shell, smooth morphology, and homogeneous structure shown by SEM images. FTIR and DSC analyses confirmed conformational changes. Entrapment efficiency and loading capacity were 96% and 50%, respectively, via direct and indirect methods. The invitro conjugate release profile, release kinetics, and mechanism of conjugate release from the nanoparticles were studied under simulated physiological conditions for various incubation periods. An initial burst effect revealed the release profile, followed by a continuous and controlled release phase. The compound release mechanism from the polymer was due to Fickian diffusion. Our results indicated the prepared nanoparticles could be appropriate for the convenient delivery of the desired conjugate.

Exploring the Advance Data Mining Tool for Optimization of Nanoparticles Laden in situ Gel for Ocular Drug Delivery

Background: Glaucoma is widely treated using eye drops, but around 95% of the drug is lost by the ocular barrier resulting in low bioavailability. The incorporation of polymeric nanoparticles into mucoadhesive polymer containing in situ gel is generally helpful in the retention of nanoparticles on the eye and improves the efficacy of the formulation Objective: The objective of the present investigation has to develop polymeric brinzolamide (BRZ) nanoparticles laden with timolol maleate (TM) in situ gel formulation. Methods: The optimized BRZ nanoparticles were prepared using PLGA by nanoprecipitation technique utilizing 32 full factorial designs (FFD). Healthy New Zealand White Rabbit (250-300 g) was used for the pharmacokinetic and pharmacodynamic study. Design of the experiment was applied to optimize formulation and validate the model. Some evaluation parameters related to BRZ nanoparticles as well as in-situ gel, have been done Results: The results of FFD reveal that the optimized condition for drugs to polymer ratio (1:7) containing 0.98 %w/v for poloxamer 188 results in higher entrapment efficiency and drug release with 156.7 nm particle size. The in-situ gel formulation has been prepared using Gelrite (0.5%w/v), and HPMC K4M (0.5%w/v) shows acceptable results with sustained drug release up to 6±0.1 h. The rabbit model's in-vivo pharmacokinetics and pharmacodynamic data showed sustained release of drugs longer than the marketed formulation. Conclusion: The proposed formulation could successfully deliver therapeutic concentrations in the eye with prolonged resident time and serve as a potential alternative for the treatment of glaucoma.

Formulation of a probiotic product using Almond gum.

The application of probiotics in food has expanded significantly, yet its viability remains a challenge. In response to this issue, this study explores a unique approach. Almond gum, a natural extract from Prunus dulcis, is utilized as the primary carrier matrix for a novel probiotic product featuring Saccharomyces boulardii, a probiotic yeast. This study involves the entrapment of S. boulardii in almond gum through centrifugation (5 min at 1300 × g) and subsequent 24 h drying at 50 °C. Sensory evaluation and other investigations were conducted at different pH levels to assess viability and performance. Post-drying entrapment efficiency was 83.85%, underscoring the benefits of choosing almond gum as a carrier matrix. Promising results were observed from viability testing conducted in gastric juice (pH 1.2) and in simulated intestinal fluid (pH 6.8). Matrix stability was assessed by measuring cfu ml-1 following 7 days' storage at different temperatures, complemented by sensory analysis. Almond gum is a promising carrier matrix for probiotic products. Its high entrapment efficiency and its viability under challenging pH conditions demonstrate its efficacy. It is rich in carbohydrates and serves a dual purpose by acting as a prebiotic source, as confirmed through ultraviolet-visible (UV-visible) analysis. The study underscores the potential of this novel approach, providing insights into responses to viability challenges in probiotic food products. © 2024 Society of Chemical Industry.

Enhancing apoptosis-mediated anticancer activity of evodiamine through protein-based nanoparticles in breast cancer cells

In the cutting-edge era of developing precision therapeutics, nanoparticles have emerged as a potent drug delivery system. Altering the size of poorly water-soluble drugs to nanoscale could confer change in their physical properties, including enhanced water solubility and bioavailability. Evodiamine (EVO), a natural indolequinone alkaloid extract from Evodia rutaecarpa, has shown several important pharmacological applications, anti-cancer being one of them. Protein-based nano-drug delivery systems have gained the interest of researchers due to their better biocompatibility, biodegradability, non-immunogenicity and non-toxicity. In the present study, EVO encapsulated BSA nanoparticles (ENPs) were synthesized and characterized, which were nanoscale-sized (~ 150 nm), monodispersed, spherical shaped, and showed high entrapment efficiency (~ 86%) and controlled drug release. The in-vitro anti-cancer activity of ENPs on human breast cancer cells was dose- and time-dependent. The apoptotic molecular mechanism investigated using FACS, qRT-PCR, and western blotting analysis, revealed increased expression of p53 and Bax and decreased expression of Bcl-2. Biological studies demonstrated comparatively more efficient and targeted delivery of ENPs than pure EVO. The comprehensive physiochemical characterization and in-vitro validation collectively pinpoint ENPs as a promising avenue for harnessing the therapeutic potential of the natural anti-cancer compound EVO. The findings indicate improved cytotoxicity, positioning ENPs as a propitious strategy for advancing breast cancer treatment.

Double W/O/W emulsion is effective for carrying calcium and vitamin D

A double emulsion is a promising system to facilitate the fortification process of nutrients such as calcium and vitamin D, as it protects vitamin D from oxidation and calcium from interactions with food proteins. The aim of this work was to produce Wi/O/We type double emulsions carrying vitamin D and calcium. The influence of the proportion of aqueous phase Wi/We (10/60, 15/55 and 20/70) and the concentration of polyglycerol polyricinoleate (PGPR) emulsifier (2.0, 2.5 and 3.0% w/w) on the kinetic stability of the emulsions over 13 days of storage was evaluated. For this, the following were analyzed: zeta potential, rheological properties (flow curve and viscoelasticity), entrapment efficiency (EE), and kinetic stability (KS) of calcium localization, microstructure, and macroscopic stability of the W/O/W emulsions, as well as the interfacial tension of the primary emulsions (Wi/O). The highest EE and KS of calcium localization were observed in treatments with smaller proportions of internal aqueous phase, regardless of the PGPR concentration. Therefore, an aqueous phase proportion of 10/60 combined with 2% PGPR is recommended.

Designing nanostructured lipid carriers modified with folate-conjugated chitosan for targeted delivery of osthole to HT-29 colon cancer cells: investigation of anticancer, antioxidant, and antibacterial activities

AbstractThe present study proposed to design nanostructured lipid carriers (NLC) coated with chitosan (CS) conjugated folate (FA) for the targeted delivery of Osthole (OST) to the HT-29 colon cancer cell line and improve its anticancer capability. To assess the physicochemical characteristics of OST-loaded NLC decorated with CS-conjugated FA (OST-NCF-NPS), several techniques, including DLS, SEM, and FTIR, were applied. After determining the encapsulation efficiency of OST in CSFA-modified NLC-NPs, an MTT test was conducted to evaluate the cytotoxic effects of this nano platform on the HT-29 cancer cell line in comparison to normal HFF cells. Possible mechanisms of apoptosis in cancer cells treated with OST-NCF-NPs were examined using qPCR, flow cytometry, and AO/PI fluorescent staining methods. Moreover, the antioxidant capacity of these biosynthesized nanocarriers was determined using ABTS and DPPH methods, and their antibacterial potential was measured through disk diffusion, MIC, and MBC assays. According to the findings, OST-NCF-NPS had the ideal average size of 179.19 nm, low polydispersity (PI = 0.23), acceptable physical stability (ζ-potential = + 18.99 mV), and high entrapment efficiency (83.5%). The MTT data demonstrated the selective cytotoxicity of NPs toward cancerous cells compared to normal cells. Cell cycle and Annexin V/Propidium Iodide (AnV/PI) analysis indicated that OST-NCF-NPs increased the sub-G1 population and AnV/PI-positive cells. The occurrence of programmed cell death in the treated cells was also verified by altered expression of proapoptotic (BAX and caspase-3) and antiapoptotic (Bcl-2) genes. Furthermore, the NPs exhibited strong antibacterial activity, particularly against gram-negative bacteria, and high antioxidant effects in reducing ABTS and DPPH-free radicals. Graphical Abstract