Search

The current study analyzes the possibility of determining the drug location in electrospun polymeric matrices and forecasting the release kinetics of drug delivery systems. Electrospun membranes made of polycaprolactone (PCL) loaded with dacarbazine (the drug of choice for the treatment of melanoma) and with AuM1 (a promising synthetic Au‐based complex recently proposed for antitumoral treatments) are successfully prepared. Atomic force microscopy (AFM) analysis is performed on various membranes, highlighting the relevance of investigating the three‐dimensional topology of the membranes for understanding the release kinetic. The produced mats are similar for all membranes, but significant differences in the microscopic roughness wall between the systems loaded with AuM1 and dacarbazine are observed. For AuM1, which has a low affinity with the PCL matrix, the complex aggregates on the nanofibers' external walls, consequently increasing the roughness and causing a high burst in the first hours of release. On the other hand, dacarbazine is successfully included in the bulk core of the PCL nanofibers. Thus, the release kinetics is diffusive and well described by the Fick model. [ABSTRACT FROM AUTHOR]

This study aims to develop a new class of versatile silica‐based materials for medical applications, synthesized via the sol–gel method. Different molecules are incorporated into the silica matrix to improve its biological properties and to use these materials as better‐performing implants. Polyethylene glycol (PEG) is added to silica‐based materials to improve biocompatibility, increase hydrophilicity, and enhance cellular adhesion and growth. The effect of loading the silica/PEG matrix with chlorogenic acid (CGA), a natural compound present in different types of plants, is investigated to understand how the material is affected. The interactions among different components in the hybrid materials are studied by Fourier‐transform infrared (FTIR) spectroscopy. Furthermore, the materials are encapsulated in 2% w/v of alginate to evaluate the different releases of CGA, using UV‐Vis Spectrophotometer. Finally, antimicrobial assessment against Escherichia coli and Pseudomonas aeruginosa of the several hybrids is observed by measuring the diameter of the zone of inhibition. [ABSTRACT FROM AUTHOR]

Poly(3-hydroxybutyric acid)-based microspheres of two types, with and without macropores, were prepared; their morphology and particle size were evaluated. These microspheres were entrapped as disperse fillers into the bulk of macroporous cryogels based on poly(vinyl alcohol) (PVA). It was found that the rigidity of the resultant composite cryogels increased markedly as compared to that of unfilled cryogels of the same PVA concentration. The resulting composites were further tested for their potential to act as drug carriers. With that, simvastatin was included into the filler particles directly in the course of their preparation, followed by entrapment of such drug-loaded microspheres into the PVA cryogel. In turn, ibuprofen sodium salt was introduced into the preliminary prepared cryogels filled with the drug-free microspheres. The experimental study of drug release kinetics showed that due to the non-covalent interactions of both simvastatin and ibuprofen sodium salt with the particles of discrete phase, prolongation of the release processes was observed.

Hydrogels have emerged as promising biomaterials due to their excellent performance; however, their biocompatibility, biodegradability, and absorbability still require improvement to support a broader range of medical applications. This paper presents a new biofunctionalized hydrogel based on in situ crosslinking between maleimide-terminated four-arm-poly(ethylene glycol) (4–arm–PEG–Mal) and poly(ε-lysine) (ε–PL). The PEG/ε–PL hydrogels, named LG–n, were rapidly formed via amine/maleimide reaction by mixing 4–arm–PEG–Mal and ε–PL under physiological conditions. The corresponding dry gels (DLG–n) were obtained through a freeze-drying technique. 1H NMR, FT–IR, and SEM were utilized to confirm the structures of 4–arm–PEG–Mal and LG–n (or DLG–n), and the effects of solid content on the physicochemical properties of the hydrogels were investigated. Although high solid content could increase the swelling ratio, all LG–n samples exhibited a low equilibrium swelling ratio of less than 30%. LG–7, which contained moderate solid content, exhibited optimal compression properties characterized by a compressive fracture strength of 45.2 kPa and a deformation of 69.5%. Compression cycle tests revealed that LG–n demonstrated good anti-fatigue performance. In vitro degradation studies confirmed the biodegradability of LG–n, with the degradation rate primarily governing the drug (ceftibuten) release efficiency, leading to a sustained release duration of four weeks. Cytotoxicity tests, cell survival morphology observation, live/dead assays, and hemolysis tests indicated that LG–n exhibited excellent cytocompatibility and low hemolysis rates (

The obtention of amorphous solid dispersions (ASDs) of mycophenolic acid (MPA) in poly(ε-caprolactone) (PCL) is reported in this paper. An improvement in the bioavailability of the drug is possible thanks to the favorable specific interactions occurring in this system. Differential scanning calorimetry (DSC) was used to investigate the miscibility of PCL/MPA blends, measuring glass transition temperature (Tg) and analyzing melting point depression to obtain a negative interaction parameter, which indicates the development of favorable inter-association interactions. Fourier transform infrared spectroscopy (FTIR) was used to analyze the specific interaction occurring in the blends. Drug release measurements showed that at least 70% of the drug was released by the third day in vitro in all compositions. Finally, preliminary in vitro cell culture experiments showed a decreased number of cancerous cells over the scaffolds containing MPA, presumably arising from the anti-cancer activity attributable to MPA. [ABSTRACT FROM AUTHOR]

The objective of this study was to develop biodegradable, environmentally friendly, economical and smart gelatin-based hydrogels and ferrogels as controlled drug delivery systems. Cross-linking is an important treatment for controlling the drug release from hydrogels, as well as enhancing the thermal and mechanical stability of hydrogels. In this study, gelatin-based hydrogels and ferrogels were synthesized at different cross-linker concentrations, ranging from 4 to 16 wt% to allow for different mesh and pore sizes in the gelatin matrix. The gels were characterized by thermogravimetric analysis, Fourier transform infrared spectroscopy, scanning electron microscopy, and energy dispersive X-ray spectroscopy. The swelling properties and in-vitro release of tetracycline as a model drug from the hydrogels and ferrogels cross-linked with different ratios by the diffusion mechanism were tested in solutions of pH 6.5 and 7.4 at 37 °C, which mimics environments similar to those of the mouth and intestines. The results showed that the swelling and drug release properties of all the gelatin hydrogels and ferrogels significantly depended on the cross-link level because of the effect of the cross-linking mechanism on reducing the number of free carboxyl and free amino groups of gelatin matrix. In addition, it was observed that the presence of magnetic nanoparticles in the gelatin matrix has an effect of decreasing the swelling and drug release percent of the gelatin-based hydrogels. [ABSTRACT FROM AUTHOR]

With the increasing use of implantable patches in biomedical applications, the significance of surface modification techniques in improving biocompatibility, enhancing adhesion, and regulating drug release has grown. A significant challenge that these methods must address is ensuring that the process does not harm the delicate fibers or therapeutic agents they contain. Here, we report surface functionalization of implantable, curcumin loaded Polycaprolactone (PCL) patches with pH‐responsive poly(2‐hydroxyethyl methacrylate‐co‐4‐vinylpyridine), p(HEMA‐co‐4VP) polymer thin film. The polymer was coated on the patch surface via photo‐initiated chemical vapor deposition (piCVD) where the polymerization was initiated by the UV degradation of the initiator tert‐butyl peroxide (TBPO) and the monomer HEMA. Additionally, the piCVD method was utilized to crosslink the HEMA without the use of additional crosslinkers. The pH‐responsiveness of the coating was achieved by incorporating 4VP into the copolymer structure. The effect of the coating was demonstrated through degradation and drug release studies. The presence of the polymer coating decelerated the fiber degradation and the pH‐dependent swelling of the coating allowed for the control of drug release rates from the patches. The innovative use of piCVD as a coating method provides a platform for advancing tailored surface modifications in various biomedical applications. [ABSTRACT FROM AUTHOR]

Background: Oral Thin Film (OTF) is an emerging approach for oral drug delivery but still there exists a scarcity of evidence for formulation optimization techniques. Herein, we aim to develop OTFs optimized by the QbD approach. Materials and Methods: OTFs were prepared by solvent casting method using Amlodipine as an active ingredient and excipients such as Pectin, Aspartame, Tween 80, and Glycerine. The developed formulation was optimized using QbD software Design Expert version 8.0.4, USA. The independent variables of the experiment were selected as A-pectin, B-Tween-80, and C-glycerine, and the dependent variables were R1-tensile strength (kg/cm2), R2-permeation rate (µg/cm2/hr), R3-disintegration time (in a sec). Finally, the software suggested optimized formulation based on a desirability value closer to 1. Results: The optimized oral films were comparatively evaluated and characterized by various techniques. The drug release was found to be ~96% at 10 min for OTFs and ~94% at 20 min for oral fast-dissolving tablets. The amlodipine was scanned in the UV range of 200 to 400 nm and the λmax was observed to be at 240±2 in a Phosphate of pH 6.8. Conclusion: All results are found satisfactory and well within the acceptance range. This ensures that similar formulations can be optimized by using this technique in the future. [ABSTRACT FROM AUTHOR]

In recent years, the use of nanoparticles in the field of medicine has attracted many attentions. The surface coating of nanoparticles by biocompatible polymers improves their bioavailability. Due to the compatibility of bio-polymers with the environment and human body, these materials are used as carrier agents. In this research, magnetic nanoparticles were synthesized by microwave and hydrothermal methods. The iron oxide nanoparticles (Fe3O4) were coated with polyvinyl alcohol (PVA) to prepare nanocomposite and load the drug (vitamin C) from the mechanical agitator. The nanoparticles crystal structure was studied using X-ray diffraction (XRD). The nanoparticles size was determined by scanning electron microscopy (SEM). Vibrating sample magnetometer (VSM) was used for magnetic analysis, and the purity of the material was determined by applying Fourier transform infrared spectrometer (FT-IR). Evaluation of drug release was investigated by ultra violet-visible (UV-Vis) spectroscopy. [ABSTRACT FROM AUTHOR]

Titanium is the optimal biomaterial for orthopedic and dental applications. Due to its biocompatibility and superior mechanical properties, it is more suitable for implant applications than other metals. However, due to its bio-inertness, the surface of titanium must be modified for human bone tissue. Various techniques can be used to construct titanium dioxide (TiO2) nanoparticles (TNPs), but anodizing is the most often used because of its portability and low cost. Due to the high similarity of hydroxyapatite to the mineral components of bone and dentin, metal implants are coated with bone-conducting biomaterials such as hydroxyapatite (HA) to enable better bone bonding. In this study, copper and chitosan were used because of their excellent antimicrobial properties. Electrochemical impedance tests show that an HA/Cu/Drug/chitosan (Chit) coating has a polarization resistance of 300,000 Ω because the copper coating on the titanium dioxide nanoparticle (TNP) increases corrosion resistance. A potentiodynamic polarization test shows that the current of corrosion of the HA/Cu/Drug/chitosan sample is 2.1719 x 10-6 A. The antibacterial activity of the HA/Drug, HA/Drug/Chit, and HA/Cu/Drug/Chit coatings was evaluated in vitro against Staphylococcus aureus ATCC 29737, and it is found that the HA/Cu/Drug/Chit coating presents high antibacterial activity due to the presence of copper and chitosan. Its optical density is 0.78, which is lower than that of all the other samples. Cell viability is highest for the TNP samples containing chitosan. Regarding the TNP sample containing HA/Drug (99.4%), it is observed that the percentage of cell viability is higher than that of the TNP sample containing HA/Cu/Drug (97.54%) due to the toxicity of copper. This study shows that the modification of the titanium implants can be used to control drug release and enhance corrosion resistance, antibacterial properties, and cell viability. [ABSTRACT FROM AUTHOR]

Dasatinib (DAS), a potent anticancer drug, has been subjected to formulation enhancements due to challenges such as significant first-pass metabolism, poor absorption, and limited oral bioavailability. To improve its release profile, DAS was embedded in a matrix of the hydrophilic polymer polyvinylpyrrolidone (PVP). Drug amorphization was induced in a planetary ball mill by solvent-free co-grinding, facilitating mechanochemical activation. This process resulted in the formation of amorphous solid dispersions (ASDs). The ASD capsules exhibited a notable enhancement in the release rate of DAS compared to capsules containing the initial drug. Given that anticancer drugs often undergo limited metabolism in the body with unchanged excretion, the ecotoxicological effect of the native form of DAS was investigated as well, considering its potential accumulation in the environment. The highest ecotoxicological effect was observed on the bacteria Vibrio fischeri, while other test organisms (bacteria Pseudomonas putida, microalgae Chlorella sp., and duckweed Lemna minor) exhibited negligible effects. The enhanced drug release not only contributes to improved oral absorption but also has the potential to reduce the proportion of DAS that enters the environment through human excretion. This comprehensive approach highlights the significance of integrating advances in drug development while considering its environmental implications. [ABSTRACT FROM AUTHOR]

The mathematical models available in DDSolver were applied to experimental dissolution data obtained by analysing carvedilol release from hypromellose (HPMC)-based matrix tablets. Different carvedilol release profiles were generated by varying a comprehensive selection of fillers and carvedilol release modifiers in the formulation. Model fitting was conducted for the entire relevant dissolution data, as determined by using a paired t-test, and independently for dissolution data up to approximately 60% of carvedilol released. The best models were selected based on the residual sum of squares (RSS) results used as a general measure of goodness of fit, along with the utilization of various criteria for visual assessment of model fit and determination of the acceptability of estimated model parameters indicating burst release or lag time concerning experimental dissolution results and previous research. In addition, a model-dependent analysis of carvedilol release mechanisms was carried out. [ABSTRACT FROM AUTHOR]

Purpose: Quantifying unencapsulated drug concentrations in tissues is crucial for understanding the mechanisms underlying the efficacy and safety of liposomal drugs; however, the methodology for this has not been fully established. Herein, we aimed to investigate the enhanced therapeutic potential of a pegylated liposomal formulation of topotecan (FF-10850) by analyzing the concentrations of the unencapsulated drug in target tissues, to guide the improvement of its dosing regimen. Methods: We developed a method for measuring unencapsulated topotecan concentrations in tumor and bone marrow interstitial fluid (BM-ISF) and applied this method to pharmacokinetic assessments. The ratios of the area under the concentration–time curves (AUCs) between tumor and BM-ISF were calculated for total and unencapsulated topotecan. DNA damage and antitumor effects of FF-10850 or non-liposomal topotecan (TPT) were evaluated in an ES-2 mice xenograft model. Results: FF-10850 exhibited a much larger AUC ratio between tumor and BM-ISF for unencapsulated topotecan (2.96), but not for total topotecan (0.752), than TPT (0.833). FF-10850 promoted milder DNA damage in the bone marrow than TPT; however, FF-10850 and TPT elicited comparable DNA damage in the tumor. These findings highlight the greater tumor exposure to unencapsulated topotecan and lower bone marrow exposure to FF-10850 than TPT. The dosing regimen was successfully improved based on the kinetics of unencapsulated topotecan and DNA damage. Conclusions: Tissue pharmacokinetics of unencapsulated topotecan elucidated the favorable pharmacological properties of FF-10850. Evaluation of tissue exposure to an unencapsulated drug with appropriate pharmacodynamic markers can be valuable in optimizing liposomal drugs and dosing regimens. [ABSTRACT FROM AUTHOR]

Progesterone (P4), commonly administered in high doses for endometrial cancer palliative management, has limitations in current delivery systems. This preliminary in vitro drug release study introduces electrospun patches to offer a new perspective on P4 delivery. The study aimed to assess the influence of the surfactant polysorbate 80 (PS80) on the release of P4 from polycaprolactone (PCL) fibers. The PS80 effects are examined to inform the fine‐tuning of the fibre generation process. Patches developed, PCL wet (with PS80) and PCL dry (without PS80), showed encapsulation efficiencies of 76% and 42%, respectively. The dose levels studied are 6.1 mg for PCL wet and 4.4 mg for PCL dry samples. Molecular studies show that higher surfactant levels improved P4‐polymer mixing, enhancing dissolution and release rates. Patches with PS80 released 66% of the drug in 17 h, while those without released only 51%. Release data best fit the Weibull model, showcasing promise for these patches in transdermal P4 delivery. This study offers a non‐invasive option compared to traditional methods and underscores the need for further research to confirm the patches' clinical effectiveness for potential use in gynecological oncology. [ABSTRACT FROM AUTHOR]

The electrospinning process was used to successfully encapsulate an anticancer drug, 5-fluorouracil (5-FU), into poly(ε-caprolactone)/gelatin (Gel) nanofiber mats (5-FU-PCL/Gel NFs). Nanofibers are recognized to be potential carriers for the delivery of anticancer drugs. One of the safest solvent systems for making PCL/Gel NF mats is the formic acid/acetic acid (FA/AA) solvent system. A compound solution jet was drawn from a customized coaxial spinneret using a high potential electric field of 20 kV. The loading of 5-FU with three different concentrations (5, 10, and 15 wt.%) improved PCL stabilization in the FA/AA system. The miscibility of the blended polymers in the electrospun nanofibers mats and 5-FU being well distributed in the nanofiber matrix was investigated using X-ray diffraction (XRD). In vitro 5-FU release from electrospun PCL/Gel NF mats revealed sustained release from the nanofiber mats, whereas slower release was found when higher concentrations of 5-FU were used. The produced electrospun PCL/Gel NF mats were studied by SEM, FTIR, TGA, and DSC. According to a study on drug release kinetics, 5-FU was released from PCl/Gel NFs in a diffusion-controlled pattern. [ABSTRACT FROM AUTHOR]

Fabrication of a suitable drug delivery system forms an attractive strategy to overcome the low bioavailability of quercetin. Poly(2-hydroxyethyl methacrylate–co-N-hydroxyethyl acrylamide), P(HEMA-co-HEAA) copolymer samples, and homopolymers of 2-hydroxyethyl methacrylate (PHEMA) and N-hydroxyethyl acrylamide (PHEAA) offer potential as quercetin delivery matrices owing to their favorable properties rendered in this study. Free radical polymerization applied under cryogenic conditions produced the polymer gels. The homopolymers and copolymers are noncytotoxic, porous, soft cryogels with surfaces resistant to protein and HCT-116 cancer cell adhesion. In vitro, quercetin release studies from samples reveal swelling-controlled, zero-order drug release at pH = 7.4 and 37 °C with high cumulative release percentages ranging from 92.03% to 94.82%. The durability of the cryogels and limited quercetin release at pH = 2.0 indicate that these cryogels are promising matrices for successfully delivering quercetin to the small intestine, where its primary absorption occurs. [ABSTRACT FROM AUTHOR]

Chitosan, an abundant natural polysaccharide, was conjugated with carbon dots (CDs) and self-polymerized with chloramphenicol (CAP) templates to synthesize CD-incorporated and molecularly CAP-imprinted polychitosan (CD-MIC). The CD-MIC was used for fluorescent sensing, dispersive sorption, and dosage release of CAP at different pH levels. The sphere of action mechanism, approved by emission and excitation fluorescence, UV–Vis absorption, and fluorescence lifetime measurements, regulated the fluorescence static quenching. By the Perrin model, the quenching extent was linearly correlated to CAP within 0.17 − 33.2 μM (LOD = 37 nM) at pH 7.0. With an imprinting factor of 3.1, the CD-MIC was more selective for CAP than CD, although it was less sensitive to CAP. The recoveries of 5.0 μM CAP from milk matrix were 95% (RSD = 2.3%) for CD-MIC probes and 62% (RSD = 4.5%) for CD. The Langmuir and pseudo-second-order models preferably described the isothermal and kinetic sorptions of CAP into the imprinted cavities in CD-MICs, respectively. The Weber − Morris kinetic model showed three stages involved in intraparticle diffusion, which was pH-dependent and gradually arduous at the later stage, and showed external diffusion partly engaged in the diffusion mechanism. The 20 − 70% of CAP formulated in CAP-embedded CD-MICs were released in 8 − 48 h. The release percentage was lower at pH 7.0 than at pH 5.0 and 9.0, but the equilibrium time was shorter. At pH 7.0, the release percentage reached 45% at 10 min and slowly increased to 51% at 24 h. [ABSTRACT FROM AUTHOR]

Skin wounds caused by burns, physical injuries, and diseases such as diabetes can lead to amputation and even death of people due to infection and lack of proper angiogenesis. In this research, a wound dressing was made using the electrospinning method from a blend of poly-caprolactone and gelatin polymers which Ciprofloxacin and Vitamin C were loaded in the polymers separately. The morphology of the structure was observed by scanning electron microscope followed by evaluation of hydrophilicity, swelling, degradation rate, tensile strength, and drug release pattern Fibroblast cell response was also considered using cytotoxicity test method. Results showed that the wound dressing fibers without drugs and containing drugs were uniform with a diameter of 1039.246 ± 96 and 1403± 406 nm, respectively. The wound dressing showed a suitable wide range of swelling ability and durability within 35 days. The tensile strength increased up to 3.5 times by addition of ciprofloxacin and vitamin C due tothe morphological changes. The presence of drugs in the system did not indicate any adverse effect on the cell's viability, and suitable proliferation and adhesion of skin fibroblast cells were observed on the surface of the sample. In addition, a combination of gelatin and polycaprolactone polymers could provide an appropriate degradation rate and release pattern without any crosslinking process, while preserving the mechanical properties and flexibility. [ABSTRACT FROM AUTHOR]

Topical drug delivery refers to the distribution of drugs to any region of the anatomy via the epidermis, vaginal route, ophthalmic path, or rectal pathway. Drugs can be delivered either regionally or intravenously. Topical compositions can be designed with diverse physicochemical characteristics, including solid, semisolid, or liquid consistencies. The manufacturing of the topical approach involves two steps: the synthesis of a drug emulsion and its inclusion into an emulgel. Emulgel is a composition that exhibits both thermodynamic stability and low interfacial tension. The substance possesses numerous advantageous characteristics, including elevated thermodynamic rigidity and enhanced permeation and is created through the combination of surfactants along with co-surfactants. Emulgel exhibits a consistent and bi-directional flow profile. Emulgel enhances the bioavailability of the medical care, hence increasing the likelihood of patients adhering to their specified dosage. In order to assess the performance of the structure, we subjected it to various tests including viscosity measurement, particle size analysis, zeta strength determination, drug concentration evaluation, stable examination, and epidermis irritant assessment, amongst other parameters. [ABSTRACT FROM AUTHOR]

Copyright of Polymer Materials Science & Engineering is the property of Sichuan University, Polymer Research Institute and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Recently, vast efforts towards sustainability have been made in the pharmaceutical industry. In conventional oil-in-water (O/W) cream formulations, various petroleum-based excipients, namely mineral oil and petrolatum, are commonly used. Natural or synthetic excipients, derived from vegetable sources, were explored as alternatives to petroleum-based excipients in prototype topical creams, with 1% (w/w) lidocaine. A conventional cream comprised of petroleum-derived excipients was compared to creams containing sustainable excipients in terms of key quality and performance attributes, physicochemical properties, and formulation performance. The petrolatum-based control formulation had the highest viscosity of 248.0 Pa·s, a melting point of 42.7°C, a low separation index at 25°C of 0.031, and an IVRT flux of 52.9 µg/cm2/h. Formulation SUS-4 was the least viscous formulation at 86.9 Pa·s, had the lowest melting point of 33.6°C, the highest separation index of 0.120, and the highest IVRT flux of 139.4 µg/cm2/h. Alternatively, SUS-5 had a higher viscosity of 131.3 Pa·s, a melting point of 43.6°C, a low separation index of 0.046, and the lowest IVRT flux of 25.2 µg/cm2/h. The cumulative drug permeation after 12 h from SUS-4, SUS-5, and the control were 126.2 µg/cm2, 113.8 µg/cm2, and 108.1 µg/cm2, respectively. The composition of the oil-in-water creams had influence on physicochemical properties and drug release; however, skin permeation was not impacted. Sustainable natural or synthetic excipients in topical cream formulations were found to be suitable alternatives to petroleum-based excipients with comparable key quality attributes and performance attributes and should be considered during formulation development. [ABSTRACT FROM AUTHOR]

The use of nanofiber patches has received considerable attention as a promising solution for overcoming challenges in drug delivery. In this study, silver nanoparticles (Ag NPs) were incorporated in chitosan (CS), hyaluronic acid (HYA), and polyvinyl alcohol (PVA) to form nanofibers (namely, the CS/HYA/PVA-Ag nanofiber) for the controllable release of curcumin (CUR). The CUR release from the CS/HYA/PVA-Ag nanofibers consistently happened sustainably. Therefore, the prepared CS/HYA/PVA-Ag nanofibers show great promise in terms of their ability to expand the field of pH-dependent transdermal drug delivery (TDD) and sustainably release drugs. Additionally, the scratch assay results of these nanofibers further support their potential applications in wound healing. [ABSTRACT FROM AUTHOR]

Chitosan (CS) can be extracted from waste fish scales through a series of chemical processes, including demineralization, deproteinization, and deacetylation. The biomaterial poly (acrylamide [AM]‐co‐acrylic acid [AA])/CS is a unique superabsorbent material synthesized through the free radical graft copolymerization method by using AM, AA, and CS powder. During synthesis, ammonium persulfate is used as an initiator, and N, N′‐methylene bisacrylamide is used as a cross‐linker. Scanning electron microscopy and Fourier transform infrared spectroscopy have been studied to know about the morphology and structure of the synthesized superabsorbent materials. The water absorbency of the material continuously increases from day 1 to day 30. The thermogravimetric analysis (TGA) and derivative thermogravimetry (DTG) of the superabsorbent material show adequate thermal stability. The X‐ray diffraction (XRD) analysis indicates that the synthesized biomaterial is virtually amorphous in nature. The percentage of biodegradability increases with time. The encapsulation efficiency of amoxicillin drugs is around 70%, which indicates that the biomaterial is highly efficient for drug release applications. The synthesized novel biomaterial is a low‐cost, eco‐friendly, and thermally stable hydrogel that can be effectively used in drug release applications. Highlights: Chitosan (CS)‐based hydrogels are highly pH‐sensitive towards drug release.The biodegradability and swelling behavior of the synthesized biomaterial were studied by adopting a suitable methodology.The novel material formed was characterized by using Fourier transform infrared spectroscopy, TGA, and Scanning electron microscopy. The encapsulation efficiency, kinetic study, and controlled drug release behavior of the amoxicillin drug were studied in solutions of simulated gastric fluid and phosphate‐buffered saline.The material developed in this study shows good performance in controlled drug delivery, and is therefore suitable for manufacturing medical devices used in drug delivery. [ABSTRACT FROM AUTHOR]

Polyethylene glycol 1000 vitamin E succinate (TPSG1000) was commonly used as absorption promoter, solubilizer, and emulsifier in drug delivery systems. In addition, TPGS1000 possessed thermosensitivity and gelling property that were not extensively studied. Hence, TPGS1000 was synthesized by Collnot method, characterized, evaluated for gelling property, and applied as the thermosensitive carrier in the study. Thin‐layer chromatography, Fourier transform infrared spectroscopy, and high‐performance liquid chromatography methods proved that the TPGS1000 was successfully synthesized. Under the condition of 4.5% sodium sulfate, 12% TPGS1000 could rapidly form stable hydrogels at 37°C. In addition, the gelling time tends to shorten with temperature increasing. It is worth noting that TPGS1000 as the carrier for loading doxorubicin displayed significant sustained release behavior. In conclusion, the study laid foundation for the application and further research of TPGS1000 in thermosensitive gel drug delivery system and provides a novel material for thermosensitive gel preparations. [ABSTRACT FROM AUTHOR]

In this study, polyvinylpyrrolidone/sodium carboxymethyl cellulose (PVP/NaCMC) microspheres containing an antibiotic agent Mupirocin (MP) were prepared. The effect of polymer/polymer ratio, cross-linking time and drug/polymer (d/p) ratio was investigated on MP release. The best condition for the release of MP was found to be 79.2%. Polyhydroxy methacrylate (pHEMA) based microsphere-cryogel composite system was prepared in a disk form using microspheres with the best drug release profile. Surface and bulk structures of cryogel disks were identified with scanning electron microscopy (SEM). The best MP release was found in 82.7% of the microsphere-cryogel composite system. [ABSTRACT FROM AUTHOR]

In this study, monodisperse spherical particles were synthesized by using hexachlorocyclotriphosphazene (HCCP) and 1-(2-Aminoethyl) piperazine (AEP) by the polycondensation reaction. Then, the surfaces of the synthesized nanospheres were functionalized with gold nanoparticles. Phz-AEP nanospheres and phz-AEP@Au nanocomposite were characterized by various methods. Drug release studies for the synthesized phz-AEP and phz-AEP@Au nanospheres were performed using a ribonucleic acid (RNA) and sodium diclofenac (NaDc). As a result of the release studies, the drug release kinetics of the nanospheres were investigated. Additionally, the antibacterial and antifungal effects of the synthesized phz-AEP and phz-AEP@Au nanocomposite spheres were tested. [ABSTRACT FROM AUTHOR]

The molecular mechanisms of mesoporous silica nanomaterial (MSN) loading by gemcitabine and ibuprofen molecules, respectively, are elucidated as functions of pore geometry. Based on a small series of MSN archetypes, we use molecular dynamics simulations to systematically explore molecule-by-molecule loading of the carrier material. Apart from predicting the maximum active pharmaceutical ingredient (API) loading capacity, more detailed statistical analysis of the incorporation energy reveals dedicated profiles stemming from the interplay of guest-MSN salt-bridges/hydrogen bonding in concave and convex domains of the silica surfaces - which outcompete interactions among the drug molecules. Only after full coverage of the silica surface, we find secondary layer growth stabilized by guest-guest interactions exclusively. Based on molecular models, we thus outline a two-step type profile for drug release from MSN networks. Subject to the MSN structure, we find 50–75 % of the API within amorphous domains in the inner regions of the pores – from which drug release is provided at constant dissociation energy. In turn, the remaining 50–25 % of drug molecules are drastically hindered from dissociation. [ABSTRACT FROM AUTHOR]

BACKGROUND: Polysaccharide hydrogel is one of the most important materials for the colon target drug release system. However, the degradation time of polysaccharide hydrogel is much longer than the retention time in the colon. The drugs are expelled from the body before being released. OBJECTIVE: In order to match the degradation of drug carriers and their retention time in the colon, a rapidly degradable konjac glucomannan (KGM) hydrogel was designed for colon target drug release. METHODS: A crosslinker containing azo bond, olsalazine, was used to prepare the rapidly degradable KGM hydrogel. The degradation and drug release of the hydrogels with different crosslinking densities in the normal buffer and the human fecal medium were studied to evaluate the efficiency of colon drug release. RESULTS: More than 50% of the KGM hydrogel by weight was degraded and more than 60% of the 5-fluorouracil (5-Fu) was released within 48 h in 5% w/v human fecal medium. CONCLUSION: The drug was released more rapidly in a simulated colon environment than in a normal buffer. Furthermore, the drug release was controlled by the degradation of the hydrogel. The KGM hydrogel containing azo crosslinker has great potential for colon drug release. [ABSTRACT FROM AUTHOR]

Poly(vinyl alcohol) (PVA) physical cryogels that contained the additives of o-, m-, and p-bis-phenols or phenol were prepared, and their physico-chemical characteristics and macroporous morphology and the solute release dynamics were evaluated. These phenolic additives caused changes in the viscosity of initial PVA solutions before their freeze–thaw processing and facilitated the growth in the rigidity of the resultant cryogels, while their heat endurance decreased. The magnitude of the effects depended on the interposition of phenolic hydroxyls in the molecules of the used additives and was stipulated by their H-bonding with PVA OH-groups. Subsequent rinsing of such "primary" cryogels with pure water led to the lowering of their rigidity. The average size of macropores inside these heterophase gels also depended on the additive type. It was found also that the release of phenolic substances from the additive-containing cryogels occurred via virtually a free diffusion mechanism; therefore, drug delivery systems such as PVA cryogels loaded with either pyrocatechol, resorcinol, hydroquinone, or phenol, upon the in vitro agar diffusion tests, exhibited antibacterial activity typical of these phenols. The promising biomedical potential of the studied nanocomposite gel materials is supposed. [ABSTRACT FROM AUTHOR]

The study objective was to design and characterise herein unreported polyologels composed of a range of diol and triol solvents and polyvinyl methyl ether-co-maleic acid (PVM/MA) and, determine their potential suitability for the treatment of periodontal and related diseases in the oral cavity using suitable in vitro methodologies. Polyologel flow and viscoelastic properties were controlled by the choice of solvent and the concentration of polymer. At equivalent polymer concentrations, polyologels prepared with glycerol (a triol) exhibited the greatest elasticity and resistance to deformation. Within the diol solvents (PEG 400, pentane 1,5-diol, propane 1,2-diol, propane 1,3-diol, and ethylene glycol), PEG 400 polyologels possessed the greatest elasticity and resistance to deformation, suggesting the importance of distance of separation between the diol groups. Using Raman spectroscopy bond formation between the polymer carbonyl group and the diol hydroxyl groups was observed. Polyologel mucoadhesion was influenced by viscoelasticity; maximum mucoadhesion was shown by glycerol polyologels at the highest polymer concentration (20% w/w). Similarly, the choice of solvent and concentration of PVM/MA affected the release of tetracycline from the polyologels. The controlled release of tetracycline for at least 10 h was observed for several polyologels, which, in combination with their excellent mucoadhesion and flow properties, offer possibilities for the clinical use of these systems to treat diseases within the oral cavity. [ABSTRACT FROM AUTHOR]

This research work aimed at the synthesis and characterization of novel xanthan gum/polyacrylamide/polyvinyl pyrrolidone (XG/PAM/PVP)-based hydrogels for the delivery of the hydrophobic drug ibuprofen. The influence of crosslinker, biopolymer, and initiator amount on the hydrogel's swelling ratio, porosity, and gel fraction was also investigated. Several techniques like Powder X-ray Diffraction (PXRD), Attenuated Total Reflection-Fourier Transform Infrared spectroscopy (ATR-FTIR), Scanning Electron Microscopy (SEM), and Thermogravimetry Analysis (TGA) were employed to characterize the synthesized hydrogels. Sol–gel analysis revealed an increase in the gel fraction with a rise in the concentration of MBA, XG, and KPS. Porosity measurements indicated a greater porosity with higher XG and KPS amounts, while porosity decreased as the MBA amount increased. Furthermore, the presence of PVP in the hydrogel was observed to greatly enhance various properties, including gel fraction, swelling ratio, porosity, drug loading, and drug release percent. Notably, under alkaline conditions (pH 7.4), the swelling ratio and release of ibuprofen were significantly increased, as compared to acidic (pH 1.2). The ibuprofen release from the XG/PAM/PVP hydrogel is governed by a Fickian diffusion mechanism, and the Korsmeyer-Peppas model serves as the most appropriate model for elucidating the drug release kinetic in both pH 1.2 and 7.4. The pH-responsive nature exhibited by the XG/PAM/PVP hydrogel highlights its potential as a drug delivery system. [ABSTRACT FROM AUTHOR]

Scaffolds based on gelatin (Gel) play a crucial role in bone tissue engineering. However, the low mechanical properties, rapid biodegradation rate, insufficient osteogenic activity and lacking anti-infective properties limit their applications in bone regeneration. Herein, the incorporation of ibuprofen (IBU)-loaded zeolitic imidazolate framework-8 (ZIF-8) in a methacrylated gelatin (GelMA) matrix was proposed as a simple and effective strategy to develop the IBU-ZIF-8@GelMA scaffolds for enhanced bone regeneration capacity. Results indicated that the IBU-loaded ZIF-8 nanoparticles with tiny particle sizes were uniformly distributed in the GelMA matrix of the IBU-ZIF-8@GelMA scaffolds, and the IBU-loaded ZIF-8 growing in the scaffolds enabled the controlled and sustained releasing of Zn2+ and IBU in pH = 5.5 over a long period for efficient bone repair and long-term anti-inflammatory activity. Furthermore, the doping of the IBU-loaded ZIF-8 nanoparticles efficiently enhanced the compression performance of the GelMA scaffolds. In vitro studies indicated that the prepared scaffolds presented no cytotoxicity to MC3T3-E1 cells and the released Zn2+ during the degradation of the scaffolds promoted MC3T3-E1 cell osteogenic differentiation. Thus, the drug-loaded ZIF-8 modified 3D printed GelMA scaffolds demonstrated great potential in treating bone defects. [ABSTRACT FROM AUTHOR]

The aim of this study was to design a tulobuterol (TUL) patch with good penetration behavior and mechanical properties. Particular attention was paid to the effect of transdermal permeation enhancers on the release process of metal ligand-based acrylic pressure-sensitive adhesive (AA-NAT/Fe3+). The type and dosage of the enhancers were screened by in vitro transdermal penetration in rat skin. The optimized formulation was evaluated in a pharmacokinetic study in rats. Furthermore, the molecular mechanism by which Azone (AZ) improves the release rate of TUL from AA-NAT/Fe3+ was investigated by FT-IR, shear strength test, rheological study, and molecular simulation. As a result, the optimized formula using AA-NAT/Fe3+ showed better mechanical properties compared to commercial products. Meanwhile, the AUC0-t and Cmax of the optimized patch were 1045 ± 89 ng/mL·h and 106.8 ± 28.5 ng/mL, respectively, which were not significantly different from those of the commercial product. In addition, AZ increased the mobility of the pressure-sensitive adhesive (PSA) rather than decreasing the drug-PSA interaction, which was the main factor in enhancing TUL release from the patch. In conclusion, a TUL transdermal drug delivery patch was successfully developed using metal-coordinated PSA, and a reference was provided for the design of metal-coordinated acrylic PSA for transdermal patch delivery applications. [ABSTRACT FROM AUTHOR]

The objective of the present study was to develop a W/O/W nanoemulsion (NE) drug delivery system loaded with punicalagin (PGN) for oral delivery and evaluate its potential in antibacterial therapy. The W/O/W PGN-NE was prepared using a two-step process by combining ultrasonic with high-energy emulsification and subsequently characterized by its droplet size, zeta potential, and morphology. The PGN-NE was further evaluated for its pH, in vitro antibacterial activity, drug release property, and cytotoxicity. The results indicated the formation of spherical, nano-sized globules of PGN-NE had a mean particle size of 45.53 ± 2.2 nm, with a PDI value of 0.22 ± 0.028, zeta potential was −4.67 ± 0.88 mV, and pH value was 5.8. In vitro antibacterial activity studies showed a significantly higher antibacterial activity of PGN-NE in comparison to free PGN, suggesting that NE can effectively improve the antibacterial effect of natural pharmaceuticals. The drug release assay demonstrated that PGN was slowly released from the NE preparation and absorbed, helping to prolong the potency and improve the bioavailability of PGN. Cytotoxicity testing showed that PGN had reduced toxicity when encapsulated in NE. Thus, the developed NE formulation of PNG exhibited a greater potential for the slow-release effect delivery and in the treatment of microbial infections with favorable safety profile. Micromorphology of W/O/W PGN nanoemulsion The W/O/W PGN-NE are uniform in size and non-adhesive, with a size distribution of 28.214 to 141.772 nm and a mean size of 45.53 ± 2.2 nm, respectively, with a PDI value of 0.22 ± 0.028. [ABSTRACT FROM AUTHOR]

Stimuli-responsive polymers can be used for various purposes due to their amazing properties within the context of controlled release systems. In this study, the aim was to prepare hydrogels that are stimulus-responsive to temperature and pH and utilize them in drug release investigations. N-Vinyl caprolactam-based polymers were synthesized and optimized based on the swelling ratio data. Both temperature and pH sensitivity, along with their respective transition values, were determined. The best sample was selected based on 5-FU encapsulation efficiency. To enhance the swelling ratio and encapsulation values, different amounts of poly-(ethylene glycol) were added to improve water swelling ratio and 5-FU release properties. All obtained samples were characterized using water swelling ratio, SEM, FTIR, and DSC analyses. Additionally, the encapsulation and release of the 5-FU drug from the hydrogels were studied. According to the results, it was understood that it could release the 5-FU drug approximately 14% when below the transition temperature and pH value, and approximately 99% when above the transition temperature and pH value. The kinetics of the drug release were thoroughly examined. The results of thekinetic study revealed a drug release pattern consistent with Fick's law. [ABSTRACT FROM AUTHOR]

The work is devoted to the creation of liquid and soft gel dosage forms of prolonged action. The main task to be solved in the work was to give certain rheological characteristics (namely, pseudoplastic behaviour and pronounced yield strength) to dosage forms based on solutions of pectin, sodium salt of carboxymethylcellulose and sodium salt of chitosan succinate, namely. The study has found that the effect of prolonging the release of the medicinal substance cefazolin from liquid and soft dosage forms based on polysaccharides is directly related to the rheological characteristics of the system and can manifest itself in two cases. First, it is possible for liquid dosage forms in the area of polymer concentrations in solution lower than the concentration at which the cell of meshes C < Ce is formed. In this case, with an increase in the polymer concentration, there is a decrease in the rate of the drug substance release, due to an increase in the adduct of the polymer-drug reaction Secondly, it is possible for soft gel forms in the region of concentrations greater than the concentration at which the cell of meshes C < Ce is formed, when using additives capable of ionotropic gel formation. Calcium and zinc salts were used as such additives in the work. It is in the case when the modifying additive is capable of forming a "bridging" bond between macromolecules and the gel formation is not accompanied by a decrease in the amount of the complex adduct of the reaction, there is a prolongation effect. If the gel is only formed by increasing the polymer content in the solution without the use of an additive, the compression of macromolecular tangles and the strengthening of intramolecular interaction between the polymer units in a concentrated solution results in a significant decrease in the amount of the polymer-drug reaction adduct and accelerated the drug release from the soft dosage form. Modification of polymer chain [ABSTRACT FROM AUTHOR]

Multifunctional fiber mats are explored as potential bioactive matrices for the development of the next generation of guided bone regeneration membranes with tunable microstructure, strength and therapeutic activity. In the present study, polycaprolactone (PCL) nanofibers with different concentrations of ascorbic acid derivatives (ascorbyl palmitate) and strontium polyphosphate nanoparticles (Sr-polyP NPs) were fabricated. The obtained PCL mats scaffolds were assessed not only for microstructure structure features, including morphological observation, hydrophilicity and tensile strength, but also in vitro water uptake, biodegradation (under enzymatic and hydrolytic conditions), bioactivity using SBF, as well as ascorbic acid release study. The observed results showed that the mean fiber diameter of the PCL fibers (388 ± 340 nm) increased with the increase in the concentration of the ASP and Sr-polyP NPs. The addition of ascorbyl palmitate caused an increase in viscosity from 40.6 ± 2.5 to 66.6 ± 2.0 cP in the case of 20% AsP/PCL; however, it caused a decrease in conductivity from 7.3 ± 0.4 to 6.38 µs, while there was an obvious increase in the viscosity and conductivity by Sr-polyP Nps addition from 40.6 ± 2.5 cP in the case of PCL only to 88.3 ± 2.5 cP in the case of PA1/SP15. The contact angle decreases from 125.9 ± 2.5° in the case of PCL only to 112 ± 4 and 102 ± 2.4° in the case of 20% loaded ascorbyl palmitate-PCL mats and 15% Sr/PCL, respectively. Moreover, the assessment of the antioxidant activity of PCL fiber mats containing 10% and 20% ascorbyl palmitate demonstrated that the 20% ascorbyl palmitate-PCL fiber mats have a higher antioxidant effectiveness compared to the 10% mats. This could be attributed to the controlled release of ascorbic acid from PCL, which occurs after 7 days. However, the highest tensile strength was observed for 5% Sr-polyP NPs-loaded PCL/AsP mats at 1.52 ± 0.51 MPa. Further increase of Sr-polyP NPs content resulted in a clear decrease of tensile strength to 1.13 ± 0.13and 0.93 ± 0.71 for 10% and 20% ascorbyl palmitate-PCL mats, respectively. Importantly, the fabricated AsP and Sr-polyP NPs-loaded PCL fiber mats showed induction of calcium phosphate deposition in SBF and the ability to sustain release of ascorbic acid over a time period of 28 d, in addition to the enhancement in cell proliferation compared to PCL only suggesting their application as a favorable synthetic matrix to amplify guided bone regeneration process. [ABSTRACT FROM AUTHOR]

Radiation chemistry presents a unique avenue for developing innovative polymeric materials with desirable properties, eliminating the need for chemical initiators, which can be potentially detrimental, especially in sensitive sectors like medicine. In this investigation, we employed a radiation-induced graft polymerization process with N-vinylcaprolactam (NVCL) to modify lignocellulosic membranes derived from Agave salmiana, commonly known as maguey. The membranes underwent thorough characterization employing diverse techniques, including contact angle measurement, degree of swelling, scanning electron microscopy (SEM), atomic force microscopy (AFM), Fourier-transform infrared-attenuated total reflectance spectroscopy (FTIR-ATR), nuclear magnetic resonance (CP-MAS 13C-NMR), X-ray photoelectron spectroscopy (XPS), and uniaxial tensile mechanical tests. The membranes' ability to load and release an antimicrobial glycopeptide drug was assessed, revealing significant enhancements in both drug loading and sustained release. The grafting of PNVCL contributed to prolonged sustained release by decreasing the drug release rate at temperatures above the LCST. The release profiles were analyzed using the Higuchi, Peppas–Sahlin, and Korsmeyer–Peppas models, suggesting a Fickian transport mechanism as indicated by the Korsmeyer–Peppas model. [ABSTRACT FROM AUTHOR]

In the 21st century, chemotherapy stands as a primary treatment method for prevalent diseases, yet drug resistance remains a pressing challenge. Utilizing electrospinning to support chemotherapy drugs offers sustained and controlled release methods in contrast to oral and implantable drug delivery modes, which enable localized treatment of distinct tumor types. Moreover, the core–sheath structure in electrospinning bears advantages in dual-drug loading: the core and sheath layers can carry different drugs, facilitating collaborative treatment to counter chemotherapy drug resistance. This approach minimizes patient discomfort associated with multiple-drug administration. Electrospun fibers not only transport drugs but can also integrate metal particles and targeted compounds, enabling combinations of chemotherapy with magnetic and heat therapies for comprehensive cancer treatment. This review delves into electrospinning preparation techniques and drug delivery methods tailored to various cancers, foreseeing their promising roles in cancer treatment. [ABSTRACT FROM AUTHOR]

5-fluorouracil (5-FU) forms the basis of many chemotherapy regimens and is one of the most common preferred chemotherapeutic drugs. In this study, the synthesis of temperature and pH responsive hydrogels in the release of 5-fluorouracil (5-FU) was studied to prevent drug release during blood circulation and uncontrolled overdose drug concentration at the tumor site. In this regard, the synthesis of temperature sensitive polymer Poly(N-vinylcaprolactam) PNVCL, temperature and pH sensitive polymers P(NVCL-co-VIm) and P(NVCL-co-VIm)/PVP hydrogels was carried out by the free radical polymerization method. DSC analysis revealed that as a result of copolymerization of PNVCL with hydrophilic 1-vinylimidazole (VIm) and polyvinylpyrrolidone (PVP), the lower critical solution temperature (LCST) increased and was close to the human body temperature. In addition, it was concluded from pH sensitivity analysis that the swelling ratios of the hydrogels changed with the medium pH. Additionally, hydrogels swelled in the acidic medium but shrunk in the alkaline medium. Accordingly, 5-FU release was investigated in different temperatures (25 °C and 37 °C) and pH (pH 5.5 and 7.4) medium and approximately 96% drug release was reached at 37 °C and pH 7.4. Consequently, P(NVCL-co-VIm)/PVP hydrogels at different pH and temperature mediums could be beneficially utilized as a material with the potential to be used in targeted drug delivery systems. [ABSTRACT FROM AUTHOR]

In the present work, nanoparticles of poly-(methyl methacrylate-co-butyl acrylate) (P-(MMA-co-BA)) and poly-(methyl methacrylate-co-vinyl acetate) (P-(MMA-co-VAc)) were synthesized by miniemulsion polymerization with the in situ encapsulation of praziquantel (PZQ) as a hydrophobic drug model. The reactions produced nanoparticles with diameters ranging from 67 ± 0.5 to 130 ± 1.1 nm, with an encapsulation efficiency of at least 99%. The glass transition temperatures (Tg's) of the produced copolymer nanoparticles were successfully reduced from 121.5 to −9.3 °C in the absence of PZQ and from 100.7 to −13.7 °C in the presence of encapsulated PZQ. In vitro release assays carried out at 37 and 50 °C showed that the rate of drug release increased with temperature, reaching maxima of 56 ± 3.7 and 38 ± 2.9% of release in 6 h for copolymers containing 40 wt % BA and 60 wt % VAc. Modeling of the available release data indicated the occurrence of an anomalous release mechanism as the driver for the drug release from the produced nanoparticles. Empirical mathematical modeling confirmed the influence of both the Tg and the test temperature on the rate of drug release. Finally, experimental results strongly suggested that PZQ exerts a plasticizer effect in the system, as confirmed by DSC analyses, suggesting the existence of specific interactions between the drug and the polymer matrix. Altogether, these results point out the occurrence of multifactorial effects on release of hydrophobic drugs from nondegradable polymer particles. [ABSTRACT FROM AUTHOR]

Intragastric floating‐retention drug delivery system (IFRDDS) could effectively prolong drug‐releasing time, achieving a good clinical efficacy of encapsulated drug. In this research, the green amphiphilic resin, shellac was adopted to fabricate a continuous network as the matrix of IFRRDS by their self‐assembly behavior triggered by H+. Meanwhile, the NaHCO3 and hydroxypropyl methyl cellulose (HPMC) acted as a forming agent and a precipitating agent to control the floating behavior, respectively, which could create a porous structure for lowering the true density of the tablet and continuously absorb water to enhance the density of tablet, respectively. Interestingly, the synergistic effect of NaHCO3 and HPMC was beneficial to the initiation of the floating of the complex tablet. By regulating tablet's constitution, we could tune the floating lag time, floating time, and drug‐release behavior of the tablet. For example, the drug‐releasing curve of the shellac‐based tablet containing 3 wt% HPMC and 10 wt% NaHCO3 presented a typical linear model, which was an ideal linear drug‐releasing system, and could float in 3 min and last for 16 h. Therefore, we successfully employed a facile strategy to fabricate a biobased IFRRDS with controlled drug‐release and tunable intragastric floating‐retention properties, which has great potential for the advanced medical industry. [ABSTRACT FROM AUTHOR]

The pharmaceutical industry has faced significant changes in recent years, primarily influenced by regulatory standards, market competition, and the need to accelerate drug development. Model-informed drug development (MIDD) leverages quantitative computational models to facilitate decision-making processes. This approach sheds light on the complex interplay between the influence of a drug's performance and the resulting clinical outcomes. This comprehensive review aims to explain the mechanisms that control the dissolution and/or release of drugs and their subsequent permeation through biological membranes. Furthermore, the importance of simulating these processes through a variety of in silico models is emphasized. Advanced compartmental absorption models provide an analytical framework to understand the kinetics of transit, dissolution, and absorption associated with orally administered drugs. In contrast, for topical and transdermal drug delivery systems, the prediction of drug permeation is predominantly based on quantitative structure–permeation relationships and molecular dynamics simulations. This review describes a variety of modeling strategies, ranging from mechanistic to empirical equations, and highlights the growing importance of state-of-the-art tools such as artificial intelligence, as well as advanced imaging and spectroscopic techniques. [ABSTRACT FROM AUTHOR]