Analysis Of Release Kinetics Research Articles

Ba‐Alginate Microspheres for Protein Encapsulation by Aerosolization

ABSTRACTThe encapsulation efficiency, release profiles, and kinetics of BSA from Ba‐alginate microcapsules with the size of 150–215 μm, prepared by aerosolization method starting from different BSA concentrations (w/v: 0.05%, 0.10%, 0.15%, and 0.30%), were investigated. The critical BSA w/v ratio was found to be 0.15%, and BSA release from both Ba‐ and Ca‐alginate microcapsules, prepared for comparison, was continued up to 25 and 3 h, respectively. Korsmeyer‐Peppas model was found to be valid for Ba‐alginate microcapsules according to release kinetics analysis. BSA‐loaded Ba‐alginate microcapsules were more durable and had a longer release profile than Ca‐alginate microcapsules. FTIR analysis of Ca‐alginate and Ba‐alginate microcapsules confirms the cross‐linking of Ca2+ and Ba2+ ions with alginate and supports the presence of BSA in BSA‐loaded Ba and Ca‐alginate microcapsules. Moreover, the developed BSA‐Ba‐alginate microcapsules did not show swelling behavior at pH = 1.2 and remained intact in sodium citrate solution until 24 h. These results demonstrate that Ba‐alginate microcapsules are resistant in the stomach environment and suitable for encapsulation of water‐soluble molecules such as BSA.

Luliconazole-loaded nanostructured lipid carrier: formulation, characterization, and in vitro antifungal evaluation against a panel of resistant fungal strains

Luliconazole (LCZ) is a topical imidazole antifungal agent with broad-spectrum activity. However, LCZ encounters challenges such as low aqueous solubility, skin retention, and penetration, which reduce its dermal bioavailability and hinder its efficacy in drug delivery. The aim of the present study was to formulate, characterize, and evaluate the in vitro antifungal efficacy of luliconazole-loaded nanostructured lipid carriers (LCZ-NLCs) against a panel of resistant fungal strains. The LCZ-NLCs were synthesized using a modified emulsification-solvent evaporation technique. Characterization involved assessing parameters such as poly-dispersity index (PDI), zeta potential, encapsulation efficiency (EE %), Field Emission Scanning Electron Microscopy (FESEM), Differential Scanning Calorimetry (DSC) analysis, and Attenuated Total Reflectance Fourier Transform Infrared (ATR-FTIR). Furthermore, in vitro drug release experiments, analysis of release kinetics, cytotoxicity assessments, and in vitro antifungal susceptibility tests were performed as part of the study. The findings indicated that LCZ-NLCs displayed nanoscale dimensions, uniform dispersion, and a favorable zeta potential. The encapsulation efficiency of LCZ in NLCs was approximately 90%. FESEM analysis revealed spherical nanoparticles with consistent shape. ATR-FTIR analysis indicated no chemical interaction between LCZ and excipients. In vitro drug release experiments demonstrated that LCZ-NLCs notably improved the drug’s dissolution rate. The stability testing confirmed consistent colloidal nanometer ranges in the LCZ-NLCs samples. Additionally, cytotoxicity tests revealed no toxicity within the tested concentration. Moreover, in vitro antifungal susceptibility tests demonstrated potent antifungal activity of LCZ-NLCs against the tested resistant fungal isolates. The study findings suggest that the LCZ-NLCs formulation developed in this research could be a promising topical treatment for superficial fungal infections, especially in cases of resistant infections. However, the study needs further ex vivo and in vivo tests to ensure safety and efficacy.

Development of mesalamine loaded-fenugreek gum decorated pectin microspheres for colonic drug delivery: Ex-vivo and in-vitro characterizations

Mesalamine (MES) is a preferred therapeutic agent for managing various colon disorders, including inflammatory bowel diseases (IBD). However, conventional oral dosage forms of MES face significant limitations, which reduce their effectiveness in managing these conditions. To overcome these challenges, advanced dosage forms of MES are essential. Fenugreek gum (FG), a natural polysaccharide with non-toxicity, ease of synthesis, biodegradability, and biocompatibility, was selected as a key component for developing a novel delivery system. Calcium ion crosslinked MES-incorporated FG-decorated pectin microspheres (FG@MES/PM) were successfully designed for colon-specific drug delivery using an ionotropic gelation technique. The microspheres exhibited favorable physicochemical characteristics, including a particle size of 586 nm, a polydispersity index of 0.348, an entrapment efficiency of 85.20 ± 1.02%, and a drug content of 98.52 ± 0.96%. Ex vivo mucoadhesion tests demonstrated strong mucoadhesive properties, highlighting the potential of FG@MES/PM to adhere effectively to the colonic mucosa. In vitro drug release studies showed a modified release profile, with 99.02 ± 1.80% MES released over 24 h. Release kinetics analysis confirmed that FG@MES/PM followed the Higuchi matrix model (R² = 0.9867), indicating diffusion-controlled release. The drug release mechanism was characterized as anomalous (non-Fickian) transport, with a release exponent (n) of 0.563. Overall, FG@MES/PM demonstrated promising potential for colon-specific drug delivery, offering sustained release and enhanced mucoadhesion. This study underscores the utility of FG for developing advanced drug delivery systems targeting the colon. Future research should explore the broader application of FG and similar natural polysaccharides in designing efficient and biocompatible colon-targeted formulations to improve therapeutic outcomes for IBD and related conditions.

Preparation and properties of thermal responsive 2,3-diethyl-5-methylpyrazine fragrance microcapsules with β-CD/CS as wall materials

2,3-Diethyl-5-methylpyrazine (DEMP) is recognized for its unique nutty scent but faces limitations due to rapid evaporation. The primary objective of this study was to explore the effect of incorporating DEMP with β-cyclodextrin (β-CD) and chitosan (CS) as wall material on the microstructure and thermal release behavior, antibacterial, and antioxidant characteristics. Initially, the microcapsules preparation process underwent optimization with embedding rate of 78.03 % through response surface by ultrasonic technique. The characterization of microcapsules was confirmed through SEM, FT-IR and TEM, with the majority exhibiting smooth and shell core structures that overlapped. Through sustained release kinetics analysis, the release of microcapsules under 80 °C, 50 °C and room temperature was more in line with the first-order kinetic and Avrami kinetic equation. The heat release kinetics analysis yielded a well-matched linear fitting curve. Additionally, microcapsules effectively suppressed the growth of S. aureus and E. coli germs, and demonstrated strong antioxidant properties, compared with DEMP. Adding 10 mg microcapsules to the Heat Not Burning (HNB) cigarette, the sensory quality was significantly improved. This discovery has the potential to pave a new route for the encapsulation of fragrance molecules, and expanding their multifunctional usages for enhancing the flavor of cigarettes and food.

Novel cinnamon essential oil-bacterial cellulose microcapsules for enhanced preservation of prefabricated meat

Bacterial cellulose, a naturally porous nanomaterial, shows significant potential in encapsulation and sustained-release applications. However, effective methods to construct bacterial cellulose microcapsules (BCM) are lacking, resulting in low embedding rates and poor slow-release effects. This study presents a novel and efficient BCM preparation strategy using mercerization to embed cinnamon essential oil (CEO). The CEO-BCM system was evaluated for its efficacy in preserving prefabricated meat. Results demonstrated that BCM, embedded with CEO through mercerization, achieved an embedding rate of 94.9 % and an average particle size of 63.7 μm. Mercerization transformed BC crystalline into cellulose type II, densifying the BCM structure, while intermolecular hydrogen bonding between BCM and CEO enhanced the stability of CEO-BCM. Release kinetics analysis indicated that CEO release was primarily diffusion-driven (Peppas-Sahlin model) with sustained release performance up to 20 days. Additionally, CEO-BCM exhibited excellent long-term antibacterial (≥81.2 % within 20 days), antioxidant, and thermal stability, effectively extending the shelf life of prefabricated meat products from 5 to 10 days. The developed BCM construction strategy not only addresses the challenges of direct BCM preparation and the limitations in core embedding and controlled release, but also enhances the stability of the CEO. This advancement further expands the application areas of bacterial cellulose (BC), and the prepared CEO-BCM system holds significant potential for food preservation applications.

Preparation and in vitro/in vivo evaluation of uniform-sized Goserelin-loaded sustained release microspheres

Sustained release microspheres loaded with goserelin are regarded as a promising candidate for treating prostate cancer and other sex hormone diseases. However, their widespread adoption has been hindered by issues such as wide particle size distribution and unstable release characteristics. To address these challenges, we employed a combination of the solid-in-oil-in-water microspheres preparation approach (S/O/W) and innovative premix membrane emulsification technology and deeply investigated the effects of four key parameters on the loaded performance of microspheres and the microscopic mechanisms behind them. With this approach, we successfully produced goserelin-loaded sustained release microspheres of narrow particle size distribution (Span 0.642), remarkable encapsulation efficiency (DL = 4.23 %, EE = 93.98 %), low initial burst release (about 0.50 % within 2 h), and compatibility with small injection needles (23-G, inner diameter 0.33 mm, outer diameter 0.64 mm, maximal force 59 N). In the animal model(administered dose, 2.4 mg·Kg−1), goserelin long-acting sustained release microspheres sustained release for over 32 days, maintaining effective concentrations above 2 ng·mL−1, and effectively reduced serum testosterone concentrations to castration levels (<1.0 ng·mL−1) by day 4, maintaining this inhibition for up to 21 days, exhibiting comparable efficacy to the positive control group. In vivo release kinetics analysis revealed that goserelin-loaded sustained release microspheres exhibited a release pattern dominated by diffusion with corrosion assistance in vivo. In summary, the systematic and comprehensive evaluation of uniform-sized goserelin-loaded sustained release microspheres has highlighted their excellent translational potential, and the study herein may provide new strategies and ideas for the development of microsphere dosage forms.

Preparation and evaluation of sustained release microspheres for the treatment of diabetic neuropathy

This study aimed to prepare and evaluate sustained release microspheres for the treatment of diabetic neuropathy using Various polymers including sodium alginate, ethyl cellulose, HPMC K100, Carbopol 934, and Eudragit L-100-55. Polymers were employed to assess their impact on several crucial parameter’s entrapment efficiency, production yield Particle size analysis, swelling index, in vitro dissolution, and release kinetics. The production yield of microspheres varied depending on the polymer used, with some polymers performing in advanced yields. Entrapment effectiveness was set up to be optimal with certain polymer combinations. Particle size analysis indicated that the microspheres were within the asked range for controlled release operations. The swelling index showed polymer-dependent lump actions. In vitro dissolution studies demonstrated sustained medicine release over time, with different polymers impacting both the release rate and profile. medicine release kinetics analysis revealed that the release followed specific models, reflecting the commerce between the microsphere matrix and the medicine.

Structure based release kinetics analysis of doxazosin mesylate sustained-release tablets using micro-computed tomography

The structures of solid dosage forms determine their release behaviors and are critical attributes for the design and evaluation of the solid dosage forms. Here, the 3D structures of doxazosin mesylate sustained-release tablets were parallelly assessed by micro-computed tomography (micro-CT). There were no significant differences observed in the release profiles between the RLD and the generic formulation in the conventional dissolution, but the generic preparation released slightly faster in media with ethanol during an alcohol-induced dose-dumping test. With their 3D structures obtained via micro-CT determination, the unique release behaviors of both RLD and the generic were investigated to reveal the effects of internal fine structure on the release kinetics. The structural parameters for both preparations were similar in conventional dissolution test, while the dissolutions in ethanol media showed some distinctions between RLD and generic preparations due to their static and dynamic structures. Furthermore, the findings revealed that the presence of ethanol accelerated dissolution and induced changes in internal structure of both RLD and generic preparations. Moreover, structure parameters like volume and area of outer contour, remaining solid volume and cavity volume were not equivalent between the two formulations in 40 % ethanol. In conclusion, the structure data obtained from this study provided valuable insights into the diverse release behaviors observed in various modified-release formulations in drug development and quality control.

Enhanced Therapeutic Potential of Liposome-Coated Bushen Jianpi Recipe for Hepatocellular Carcinoma.

Hepatocellular carcinoma (HCC) poses a major healthcare burden globally. Traditional Chinese medicine formula Bushen Jianpi (BSJP) recipe shows inhibitory effects on HCC but suffers from low bioavailability. This study aims to develop a BSJP-loaded liposome (BSJP@Lip) for targeted HCC treatment. BSJP@Lip was prepared using a microfluidic device. Particle characterization included size, morphology, drug loading, encapsulation efficiency, and release kinetics analysis. In vitro cytotoxicity, cellular uptake, apoptosis, and protein expression were evaluated in hepG2, Smmc-7721, and hepa 1-6 hepatic cancer cell lines treated with BSJP@Lip. BSJP@Lip nanoparticles showed a uniform spherical shape with an average size of 50 nm and zeta potential at around -2.24 mV. They significantly inhibited cell viability and induced apoptosis in a dose-dependent manner compared with traditional decoction formulations. Enhanced cellular uptake of BSJP@Lip increased the expression of proinflammatory factors IL-18 and NLRP3. BSJP@Lip nanoparticles were found to be efficiently internalized by hepatic cancer cell lines, resulting in a dose-dependent inhibition of cell viability and induction of apoptosis. This effect was accompanied by the upregulation of IL-18 and NLRP3.

Cyclodextrin grafted chitosan thermosensitive hydrogel using dual gelling agents: Drug delivery and antibacterial materials

In this paper, three kinds of cyclodextrin-grafted-chitosan (CD-g-CS) were synthesized from chitosan (CS) and β-cyclodextrin (β-CD) with different ratios. And a series of hydrogel with good temperature sensitivity and injectability were prepared by using sodium glycerophosphate (GP) and ammonium hydrogen phosphate (AHP) as dual gelling agents. The gelation formation time of hydrogel was short, and the shortest time was 0.75 min. The FTIR spectrum and 1H-NMR spectrum showed the structure of the compounds and intermolecular interactions. The molecular docking technique probed the encapsulation mechanism of the drug with β-CD. The SEM results showed that the hydrogel had a highly interconnected three-dimensional spatial structure. The swelling ratio of hydrogel was not less than 150 % within 1 h and the degradation rate of hydrogel was not less than 75 % within 14 days. The in vitro drug release results showed that the hydrogel had optimal sustained release effect, and the cumulative release ratio was 58.3 % in 34 h. The release kinetics analysis exhibited that the hydrogel conformed to the Riter-Peppas model. The hemocompatibility test and cytotoxicity test proved that the hydrogel had good biocompatibility and biosafety. The antibacterial experiments showed that the hydrogel could inhibit the biological activity of Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). Therefore, the CD-g-CS/GP-AHP hydrogel has a broad application prospect in the biological fields of drug delivery and antibacterial materials.

Stability and Retention of Nanoemulsion Formulations Incorporating Lavender Essential Oil

Lavender essential oil (LEO) is applied topically for its soothing properties, serving not only as an antiseptic in wound care but also as an insect repellent. This study investigates the impact of carrier systems on LEO encapsulation, stability, and release kinetics for potential skincare applications. The LEO carrier impact on skin hydration and barrier function was also evaluated. Conventional emulsions (CEs) and nanoemulsions (NEs) with (CELs and NELs, respectively) and without LEO incorporation were analyzed for physicochemical properties, stability, and release mechanisms. The droplet size distribution and ζ-potential remained consistent in both CE and CEL, showing the minimal influence of LEO on those parameters. NE and NEL exhibited enhanced stability and higher LEO retention compared to CE and CEL (37.38 mg/mL ± 0.48 mg/mL and 50.96 mg/mL ± 2.00 mg/mL, respectively, p &lt; 0.05), suggesting NE as a superior carrier system for LEO delivery. NEL retained LEO over 60 days at 4 °C without a significant reduction while CEL showed a notable reduction of 94.93% ± 0.08%. Release kinetics analysis showed zero-order release kinetics of LEO from both CEL and NEL (R2: 0.973 and 0.952, respectively), revealing a diffusion-based mechanism, particularly evident in NE formulations, supporting the controlled and sustained release of LEO constituents. NEL also promoted quicker skin barrier repair and enhanced skin hydration, sustaining effects for up to 120 min post application, surpassing CEL’s performance. These findings contribute to understanding the carrier system effects on LEO delivery and underscore NE as a promising vehicle for skincare applications. Further research should explore underlying mechanisms and conduct long-term safety and efficacy studies to fully exploit the therapeutic potential of NE in dermatological applications.

Enhanced delivery of doxorubicin for breast cancer treatment using pH-sensitive starch/PVA/g-C3N4 hydrogel

This study introduces a starch/PVA/g-C3N4 nanocarrier hydrogel for pH-sensitive DOX delivery in breast cancer. DOX was loaded into the nanocarrier with 44.75 % loading efficiency and 88 % Entrapment Efficiency. The release of DOX from the starch/PVA/g-C3N4 hydrogel was pH-sensitive: DOX was released faster in the acidic environment pertinent to cancer tumors (with a pH level of 5.4) than in the surrounding regular tissue environment carrying a more neutral environment (pH 7.4). The release kinetics analysis, encompassing zero-order, first-order, Higuchi, and Korsmeyer-Peppas models, revealed significant fitting with the Higuchi model at both pH 5.4 (R2 = 0.99, K = 9.89) and pH 7.4 (R2 = 0.99, K = 5.70) levels. Finally, we found that hydrogel was less damaging to healthy cells and more specific to apoptotic cells than the drug's free form. The starch/PVA/g-C3N4 hydrogel had low toxicity for both normal cells and breast cancer cells, whereas DOX loaded into the starch/PVA/g-C3N4 hydrogel had higher toxicity for cancer cells than the DOX-only control samples, and led to specific high apoptosis for cancer cells. The study suggests that DOX can be loaded into a starch/PVA/g-C3N4 hydrogel to improve the specificity of the drug's release in cancer tumors or in vitro breast cancer cells.

Modulating the release of bioactive molecules of human mesenchymal stromal cell secretome: Heparinization of hyaluronic acid-based hydrogels

An amine derivative of hyaluronic acid (HA) was crosslinked to obtain a 3D dried sponge. The sponge was subsequently rehydrated using secretome from human mesenchymal stromal cells (MSCs), resulting in the formation of a hydrogel. The release kinetics analysis demonstrated that the hydrogel effectively sustained secretome release, with 70% of the initially loaded wound-healing-associated cytokines being released over a 12-day period. Tuning the hydrogel properties through heparin crosslinking resulted in a biomaterial with a distinct mechanism of action. Specifically, the presence of heparin enhanced water uptake capacity of the hydrogel and increased its sensitivity to enzymatic degradation. Notably, the heparin crosslinking also led to a significant retention of cytokines within the hydrogel matrix. Overall, the secretome-rehydrated HA hydrogel holds promise as a versatile device for regenerative medicine applications: the non-heparinized hydrogel may function as a biomaterial with low reabsorption rates, sustaining the release of bioactive molecules contained in MSC secretome. In contrast, the heparinized hydrogel may serve as a depot of bioactive molecules with faster reabsorption rates. Given its patch-like characteristic, the HA-based hydrogel appears suitable as topical treatment for external organs, such as the skin.

Controlled delivery of 5-fluorouracil from monodisperse chitosan microspheres prepared by emulsion crosslinking.

This work aims to determine the optimal conditions for emulsion cross-linking of chitosan (CHS) with various molecular weights using glutaraldehyde as a cross-linking agent to produce 5-fluorouracil-loaded CHS microspheres (5-FU/CHS). Their drug loading and encapsulation efficiencies are found to be in the range of 3.87-12.35% and 20.13-70.45%, respectively. The dynamic light scattering results show that 5-FU/CHS microspheres are micron-sized with a uniform size distribution, and the scanning electron microscopy results show that they are spherical. The results of thermogravimetric analysis, X-ray diffraction, and Fourier transform infrared spectroscopy demonstrate that 5-FU is successfully incorporated into the microspheres. The in vitro release tests show that 5-FU/CHS have a prolonged, pH-responsive release pattern of 5-FU, and the cumulative release rate under acidic condition is much larger than that under neutral conditions. The drug release kinetic analysis further demonstrates that the release of 5-FU can be well described by the Fickian diffusion model.

Development and Characterization of Polymeric Microsponge as a New Vehicle to Deliver Urea Topically.

Topical delivery of therapeutic agents is considered beneficial due to various advantages like ease of administration, avoidance of the first-pass effect, and improved patient compliance. Therefore, scientists around the globe are exploring this route for the delivery of drugs nowadays. The present patent investigation aimed to prepare, optimize, and characterize the urealoaded microsponges for efficient topical delivery in vitro. Urea-loaded ethylcellulose microsponges were prepared using quasi emulsion solvent diffusion technique and optimized using Box-Behnken design (BBD). Furthermore, they were characterized in-vitro using various techniques like scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), and X-ray diffraction analysis (XRD). In-vitro drug release and release kinetics analysis was also performed. Urea-loaded microsponges were spherical and porous. Optimized urea loaded microsponges showed a minimum size (39.78 ± 1.98 μm), high entrapment (74.56 ± 2.8%), acceptable polydispersity index (PDI) (0.224 ± 0.081) and zeta potential (-21.9 ± 2.9 mV). These microsponges were capable of sustaining the release of urea for 24 h (91.21 ± 5.20%), and the mechanism of release was the combination of diffusion and erosion. The developed microsponge system could be beneficial for topical delivery of urea as it could reduce the dosing frequency of urea and increase patient compliance through its sustained release.

Nutrient controlled release performance of bio-based coated fertilizer enhanced by synergistic effects of liquefied starch and siloxane

The porous structure and hydrophilicity of coating shells affect the nutrient controlled-release performance of castor oil-based (CO) coated fertilizers. In order to solve these problems, in this study, the castor oil-based polyurethane (PCU) coating material was modified with liquefied starch polyol (LS) and siloxane, and a new coating material with cross-linked network structure and hydrophobic surface was synthesized, and used it to prepare the coated controlled-release urea (SSPCU). The results demonstrated that the cross-linked network formed by LS and CO improved the density and reduced the pores on the surface of the coating shells. The siloxane was grafted on the surface of coating shells to improve its hydrophobicity and thus delayed water entry. The nitrogen release experiment indicated that the synergistic effects of LS and siloxane improved the nitrogen controlled-release performance of bio-based coated fertilizers. Nutrient released longevity of SSPCU with 7 % coating percentage reached >63 days. Moreover, the nutrient release mechanism of coated fertilizer was further revealed by the analysis of the release kinetics analysis. Therefore, the results of this study provide a new idea and technical support for development of efficient and environment-friendly bio-based coated controlled-release fertilizers.

A novel pH-responsive nanoniosomal emulsion for sustained release of curcumin from a chitosan-based nanocarrier: Emphasis on the concurrent improvement of loading, sustained release, and apoptosis induction.

Curcumin application as an anti-cancer drug is faced with several impediments. This study has developed a platform that facilitates the sustained release of curcumin, improves loading efficiency, and anti-cancer activity. Montmorillonite (MMT) nanoparticles were added to chitosan (CS)-agarose (Aga) hydrogel and then loaded with curcumin (Cur) to prepare a curcumin-loaded nanocomposite hydrogel. The loading capacity increased from 63% to 76% by adding MMT nanoparticles to a chitosan-agarose hydrogel. Loading the fabricated nanocomposite in the nanoniosomal emulsion resulted in sustained release of curcumin under acidic conditions. Release kinetics analysis showed diffusion and erosion are the dominant release mechanisms, indicating non-fickian (or anomalous) transport based on the Korsmeyer-Peppas model. FTIR spectra confirmed that all nanocomposite components were present in the fabricated nanocomposite. Besides, XRD results corroborated the amorphous structure of the prepared nanocomposite. Zeta potential results corroborated the stability of the fabricated nanocarrier. Cytotoxicity of the prepared CS-Aga-MMT-Cur on MCF-7 cells was comparable with that of curcumin-treated cells (p< 0.001). Moreover, the percentage of apoptotic cells increased due to the enhanced release profile resulting from the addition of MMT to the hydrogel and the incorporation of the fabricated nanocomposite into the nanoniosomal emulsion. To recapitulate, the current delivery platform improved loading, sustained release, and curcumin anti-cancer effect. Hence, this platform could be a potential candidate to mitigate cancer therapy restrictions with curcumin.

Physicochemical properties, antioxidant activities and in vitro sustained release behaviour of co-encapsulated liposomes as vehicle for vitamin E and β-carotene.

In this study the potential of liposomes as a vitamin E (VE) and β-carotene (βC) delivery system was examined. The co-encapsulated liposomes of βC and VE (L-VE-βC) were prepared and characterized. Their antioxidant properties were evaluated by free radical scavenging activities of 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), hydroxyl radical and lipid peroxidation assay. The in vitro sustained release behaviour was then investigated and discussed. VE and βC were co-encapsulated in liposomes with high encapsulation efficiency, up to 92.49% and 86.16% for βC and VE, respectively. The antioxidant activities of L-VE-βC samples were significantly higher than that of single loaded liposome. Among different ratios of VE/βC, L-VE-βC at 5:3 exhibited the highest radical scavenging rates, with 66.80%, 56.58% and 34.39% for DPPH, ABTS and OH radical, respectively. L-VE-βC samples also had a good ability to inhibit lipid peroxidation, especially the sample with ratios of VE/βC at 5:3 and 3:1. In simulated gastrointestinal release, L-VE-βC exhibited an excellent sustained release behaviour in SGF with the accumulated rate at about 20%, while the release rate in SIF increased to over 80%, where they should be absorbed. The release kinetics analysis indicated that βC was released in the Higuchi model in stomach, and the Korsmeyr-Peppas model in intestine. Compared to single loaded liposomes, the combined-loaded liposomes exhibited higher antioxidant activity and bioavailability, suggesting the potential applications in functional foods. © 2022 Society of Chemical Industry.

In situ preparation of alendronate-loaded ZIF-8 nanoparticles on electrospun nanofibers for accelerating early osteogenesis in osteoporosis

Applying guided bone regeneration membrane (GBRm) to treat bone defects in osteoporotic patients remains a challenge, as they cannot restore the fundamental balance between osteoblasts and osteoclasts, resulting in the ineffectiveness of osteoporotic bone injury treatment. Herein, a multifunctional polycaprolactone/gelatin (PG)-blended membrane embedded with alendronate-loaded zeolitic imidazolate framework-8 (Aln/Zif-8) nanoparticles was fabricated by electrospun technique and a simple solution-phase synthesis. Surface characterizations confirmed the successful synthesis of PG/Aln-Zif-8 nanofibers endowed with excellent mechanical strength. The release kinetics analysis showed the synergistic effects of the coordination bonds among Aln, zinc ions (Zn2+), and organic ligands played a critical role in regulating the initial burst release and delayed release of Aln and Zn2+, respectively. The in vitro results of MC3T3-E1 and RAW264.3 cells demonstrated that the PG/Aln-Zif-8 membranes possessed superior anti-osteoporosis and osteoinductive properties. Furthermore, the PG/Aln-Zif-8 samples also exhibited significant bactericidal properties against both Staphylococcus aureus and Escherichia coli. The in vivo results further confirmed that PG/Aln-Zif-8 membranes had superior osteoinduction abilities, contributing to the accelerated osseointegration in the osteoporosis model. Altogether, these new bioinspired surface modifications highlight the promising alternative for fabricating multifunctional MOFs on electrospun membranes to accelerate early osteogenesis in osteoporosis.

Sustained release matrix tablet of 100 mg losartan potassium: Formulation development and in vitro characterization

Sustained release matrix tablets of 100 mg losartan potassium HCl were fabricated with two release retarding polymers namely HPMC K100 M and affinisol by direct compression method. Nine trial formulations were prepared by varying content of these polymers, each from 50 mg to 100 mg; keeping the total weight of the tablet 310 mg. The best formulation was selected based on in vitro drug release profile for 12 hours conducted in Type II dissolution apparatus at 50 rpm and water as dissolution medium. Pre-compression parameters such as bulk density, tap density, Carr’s index and Hausner ratio were evaluated for the selected tablet. The tablets were subjected to thickness, weight variation test, drug content, hardness and friability. Drug release kinetics, surface morphology and accelerated stability study were investigated for that selected formulation. Formulation F4 with the composition of 75 mg HPMC K100M and 100 mg affinisol was selected as the best formulation that extended the drug release up to 12 hours. Pre-compression parameters and other tableting properties were within the Pharmacopoeia limit. Release kinetics analysis proved non-fickian zero-order drug release and that was further confirmed by surface morphology of the tablets before and after dissolution study visualized by SEM. The developed formulation was found to be stable for one month stored at 60 ○C.