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Aim: The goal of the present study was to develop and optimize loxoprofen-loaded microspheres for sustained-release drug delivery system. Loxoprofen is a potent NSAID prodrug belonging to the BSC class II drug with high permeability and low solubility. It is utilized to treat long-term pain and inflammatory disorders. Methods: Microspheres were developed using the protein gelation technique, with varying concentrations of egg albumin and Tween 80 as suggested by the Box-Behnken design. The spherical morphology of the microspheres was confirmed through Scanning electron microscopy. The formulation with the most desirable size of particle and entrapment efficacy was chosen. Results: The microspheres exhibited a particle size (PS) of 191.27nm and entrapment efficacy (EE) of 78.98%, with a low deviation. Batch F9 showed the optimal results. In vitro investigations showed that pure LOX was released completely within 1 hour, while LOX-loaded microspheres released 88.07% within 8 hours. The formulation exhibited short-term stability, maintaining its integrity and properties when stored at room temperature. Conclusion: Loxoprofen-loaded egg albumin microspheres can be a potential sustained-release drug delivery, offering a controlled and prolonged release of therapeutically active drug concentrations at the target site.

Background Loxoprofen has been actively used clinically to relieve musculoskeletal pain and inflammatory symptoms. However, there are few reports on quantitative pharmacokinetic (PK) prediction tools and diversity analyzes for loxoprofen within populations. Objectives The aim of this study was to identify effective covariates associated with explaining inter-individual PK variability through a population pharmacokinetic (Pop-PK) modeling approach for loxoprofen, and to provide a starting point for establishing scientific dosing regimens. Method The bioequivalence PK results of loxoprofen performed on 52 healthy Korean men and the physiological and biochemical parameters derived from each individual were used as base data for the development of a Pop-PK model of loxoprofen. In order to simultaneously predict the PKs of the active form according to loxoprofen exposure, previously reported PK results of trans-alcohol loxoprofen, an active metabolite of loxoprofen, were used to expand the model. Results The Pop-PK profiles of loxoprofen were described in terms of the basic structure of a non-sequential two absorption with 2-disposition compartment, and for inter-individual PK variations, peripheral compartment volume of distribution could be correlated with body surface area (BSA), and central compartment clearance with creatinine clearance (CrCL) and albumin levels. As a result of the model simulation, the concentrations of loxoprofen and its alcoholic metabolites in plasma significantly decreased as CrCL and albumin levels increased and decreased, respectively. On the other hand, it was confirmed that the higher the BSA, the greater the distribution of loxoprofen to the periphery, and the minimum concentrations of loxoprofen and alcoholic metabolites in plasma in steady-state increased by approximately 1.78–2 times, while the fluctuation between maximum and minimum concentrations decreased. The results suggest that patients with large BSA, impaired renal function, and high serum albumin levels may have significantly higher plasma exposure to loxoprofen and trans-alcohol loxoprofen. It was also suggested that the potential side effects in the gastrointestinal system and various tissues and the level of exposure in plasma due to long-term application of loxoprofen in this patient group could be causally explained. Conclusion This study provides a very useful starting point for a scientific precision medicine approach to loxoprofen by discovering effective covariates and establishing a quantitative model that can explain the diversity of loxoprofen PKs within the population. Clinical trial registration The clinical study protocol used in this study was thoroughly reviewed and approved by the Institutional Review Board of the Institute of Bioequivalence and Bridging Study, Chonnam National University, Gwangju, Republic of Korea. The bioequivalence study permit numbers are as follows: 041113; 10.15.2004. Graphical abstract

To formulate and evaluate ethosomes for the transdermal delivery of loxoprofen, a potent non-steroidal anti-inflammatory drug (NSAID). Fifteen ethosomal formulations were created via thin-film hydration and probe sonication techniques, with variations in the amounts of egg yolk lecithin, ethanol, cholesterol (CHOL), Tween 80 (TW80), and propylene glycol (PG). The formulations were assessed for their particle size (PS), zeta potential (ZP), polydispersity index (PDI), pH, and entrapment efficiency (EE). Field scanning electron microscopy (FSEM) was utilized to evaluate their morphology. The drug release and permeability of the ethosomal formulations were evaluated against those in a hydroethanolic drug solution. The formulation labeled F14, comprising 1% loxoprofen, 1% egg yolk lecithin, 30% ethanol, 5% propylene glycol, and phosphate-buffered saline (PBS) up to 25 ml, was recognized as an optimized ethosomal formulation. These ethosomes demonstrated an average size of 164.2±19 nm, a PDI of 0.280±0.028, a ZP of +45.1±4.5 mV, and an EE of 96.8±0.43%. and tests demonstrated that the ethosomal formulation (F14) showed superior drug release and penetration rates compared to a conventional hydroalcoholic solution. The differential scanning calorimetry (DSC) study showed that loxoprofen was completely trapped within ethosomes. On the other hand, the Fourier transform infrared (FTIR) study confirmed that the drug and the additives did not interact. The current study revealed that loxoprofen can be effectively delivered transdermally via the ethosomal system.

Industrial-based application of supercritical CO2 (SCCO2) has emerged as a promising technology in numerous scientific fields due to offering brilliant advantages, such as simplicity of application, eco-friendliness, and high performance. Loxoprofen sodium (chemical formula C15H18O3) is known as an efficient nonsteroidal anti-inflammatory drug (NSAID), which has been long propounded as an effective alleviator for various painful disorders like musculoskeletal conditions. Although experimental research plays an important role in obtaining drug solubility in SCCO2, the emergence of operational disadvantages such as high cost and long-time process duration has motivated the researchers to develop mathematical models based on artificial intelligence (AI) to predict this important parameter. Three distinct models have been used on the data in this work, all of which were based on decision trees: K-nearest neighbors (KNN), NU support vector machine (NU-SVR), and Gaussian process regression (GPR). The data set has two input characteristics, P (pressure) and T (temperature), and a single output, Y = solubility. After implementing and fine-tuning to the hyperparameters of these ensemble models, their performance has been evaluated using a variety of measures. The R-squared scores of all three models are greater than 0.9, however, the RMSE error rates are 1.879 × 10−4, 7.814 × 10−5, and 1.664 × 10−4 for the KNN, NU-SVR, and GPR models, respectively. MAE metrics of 1.116 × 10−4, 6.197 × 10−5, and 8.777 × 10−5errors were also discovered for the KNN, NU-SVR, and GPR models, respectively. A study was also carried out to determine the best quantity of solubility, which can be referred to as the (x1 = 40.0, x2 = 338.0, Y = 1.27 × 10−3) vector.

Aim: The present study deals with development and validation of accurate, sensitive and cost-effective RP-HPLC method for Loxoprofen sodium. Method: PRIMESIL C18 column (id 4.6 x 250 mm length) was used as stationary phase and a mobile phase used was mixture of methanol and 0.05% OPA buffer in ratios of 75:25 v/v. The 20µl samples were injected at a flow rate of 1 ml/min. The detector used is G-13148 (DAD) detector, with a wavelength observed of 225nm at ambient column temperature. Further, the method developed was validated as per ICH guidelines. Results: The method's linearity was studied at concentrations between 5 and 25µg/ml, wherein the results were found to be linear with correlation coefficient (r2) values of 0.999. The limits of detection and quantitation for developed method were observed to be 0.09175 and 0.278032 µg/ml respectively. The intraday and interday precision results were analysed and found to be within 2%. The percentage assay of the marketed product was found to be 101.85±0.090%. The percentage recovery of the drug was ranged between 97.7 1% to 101.09%. during accuracy study.

The objective was to develop naturally derived polymer-based hydrogels with high mechanical strength and a controlled delivery of drug for extended period of time. Here, we report the fabrication of chemically cross-linked polyvinyl alcohol- graft -poly(acrylic acid)/sodium alginate hydrogel as a semi-interpenetrating polymer network (SIPN). For the preparation of SIPN hydrogels, SA and PVA were cross-linked with AA monomer in the presence of co-monomer EGDMA through free-radical polymerization reaction, using APS as an initiator. Loxoprofen sodium was loaded as a model drug. FTIR, XRD, TGA, and DSC were performed for the characterization of copolymer. Surface morphology was studied by SEM. Swelling studies were carried out at low and higher pH to evaluate pH-dependent swelling of formed SIPN hydrogels. FTIR, XRD, TGA, and DSC studies confirmed the formation of a new copolymer. Developed SIPN hydrogels showed maximum swelling, drug loading, and drug release at pH 7.4 while low at pH 1.2. Moreover, formulations with higher AA contents showed maximum swelling at 7.4 pH. High drug loading and higher drug release have been observed at pH 7.4. In vitro release profile of loxoprofen sodium was found dependent on pH, concentration of monomers, and cross-linking agent. Gel% and yield% for the prepared SIPN hydrogels were determined and found that gel% or yield% is directly proportional to the concentration of polymers, i.e., SA and PVA, due to their behavior as macromolecule radicals for monomer. The results from FTIR analysis showed that both SA and PVA react with the acrylic acid monomer during the polymerization process and result into the formation of SIPN. The formation of semi-IPN structure significantly improved the surface morphology of SIPN hydrogels as evident by SEM, which corresponds to their improved swelling ability and mechanical strength. Drug release mechanism from the formed SIPN was explained by kinetic modeling and found that first-order, Higuchi model, and Korsmeyer–Peppas model are the best fit models to explain drug release from hydrogels. Conclusively, prepared hydrogels were highly pH-responsive and showed good mechanical strength and time-dependent drug release. SIPN hydrogels could be a potential carrier network for controlled delivery of loxoprofen sodium for extended period of time.

The majority of newly developed drugs need to be incorporated with delivery systems to maximize their effect and minimize side effects. Nanoemulsions (NEs) are one type of delivery system that helps to improve the solubility and dissolution of drugs, attempting to enhance their bioavailability and onset of action. The objective of this investigation was to develop an omega-3 oil-based NE loaded with loxoprofen (LXP) to enhance its dissolution, in vitro release, and mucosal penetration and decrease its mucosal ulcerative effects when applied in an oral treatment. LXP-loaded NEs were formulated with varying levels of omega-3 oil (10-30%), surfactant polyoxyethylene-C21-ethers (laureth-21) (40-60%), and co-surfactant polyethylene glycol-40 hydrogenated castor oil (HCO-40) (30-50%) using an extreme vertices mixture design. The developed NEs were characterized for globule size and drug loading capacity. The optimal formulation was tested for in vitro drug release, ex vivo permeation, and ulcer index value. The developed NE acquired a globule size ranging 71-195 nm and drug loading capacity of 43-87%. Considering the results of the in vitro release study, the optimized NE formulation achieved 2.45-fold and 2-fold increases in drug permeation across tested mucosa compared to a marketed tablet and drug aqueous dispersion, respectively. Moreover, the optimum NE exhibited the best ulcer index in comparison to drug aqueous suspension and different formulations when tested in rats. Overall, this research highlights the capacity of NEs to deliver LXP with enhanced solubility, drug release, and permeation while effectively protecting the application site from side effects of the model drug.

Rheumatoid arthritis (RA) is an autoimmune disease of synovial inflammation that affects populations worldwide. Transdermal drug delivery systems for treating RA have increased but remain challenging. We fabricated a dissolving microneedle (MN) system with photothermal (PT) polydopamine (PDA) to co-load the non-steroidal anti-inflammatory drug loxoprofen (Lox) and the Janus kinase inhibitor tofacitinib (Tof), with the aim of co-delivering Lox and Tof directly to the articular cavity, aided by the combination of MN and PT. In vitro and in vivo permeation studies showed that the PT MN significantly promoted drug permeation and retention in the skin. An in vivo visualization of the drug distribution in the articular cavity showed that the PT MN significantly promoted drug retention in the articular cavity. Importantly, compared to the intra-articular injection of Lox and Tof, the application of the PT MN to a carrageenan/kaolin-induced arthritis rat model exhibited superior performance in reducing joint swelling, muscle atrophy, and cartilage destruction. Furthermore, the PT MN downregulated the mRNA expression levels of proinflammatory cytokines, including TNF-α, IL-1β, iNOS, JAK2, JAK3, and STAT3. The results show that the PT MN transdermal co-delivery of Lox and Tof is a new synergetic therapy with high compliance and good therapeutic efficacy for RA.

BackgroundChronic Non-Specific Low Back Pain (CNLBP) is a prevalent musculoskeletal condition. Tuina therapy and non-steroidal anti-inflammatory drugs (NSAIDs) are two commonly used treatments for CNLBP, both of which have demonstrated some clinical efficacy. However, the effectiveness, safety, and potential opioid-sparing effects of Tuina, a classic complementary and alternative therapy, have yet to be rigorously validated through clinical research.ObjectiveThis study aims to conduct a randomized controlled superiority trial with an open-label design, blinded assessment, and parallel groups to evaluate the effectiveness, safety, and complementary role of Tuina in the treatment of CNLBP.Study design and methodsThis is a single-center, randomized controlled, assessor-blind clinical trial. A total of 80 participants aged 18–60 years meeting the diagnostic criteria for CNLBP will be recruited and randomly assigned to either the experimental group (Tuina combined with Loxoprofen Sodium patches) or the control group (Loxoprofen Sodium patches). The Tuina intervention will be administered three times weekly for four consecutive weeks; Loxoprofen Sodium patches will be used as needed. The primary outcome measure is the Visual Analogue Scale (VAS) for pain after 4 weeks of treatment. Secondary outcomes include the Oswestry Disability Index (ODI), 36-Item Short Form Health Survey (SF-36), Beck Depression Inventory-Second Edition (BDI-II), Beck Anxiety Inventory (BAI), Surface Electromyography (sEMG) and musculoskeletal ultrasound (MSK US) parameters, medication usage, and 12-week follow-up data. Statistical analysis will follow the intention-to-treat (ITT) principle, using SPSS 26.0 for between-group comparisons and repeated measures analysis.DiscussionThrough a rigorous randomized controlled design incorporating both physiological and morphological objective indicators, this study aims to provide high-level evidence regarding the analgesic efficacy, safety, and potential for drug dose reduction of Tuina in treating CNLBP. It also seeks to offer clinical evidence and practical references for the application of Tuina in the rehabilitation of musculoskeletal disorders.Clinical trial registrationhttps://itmctr.ccebtcm.org.cn/mgt/project/user/user-project-view/4621255a-332d-4ba4-b09b-e9412ba06d0b, Identifier (ITMCTR2026000745).

BACKGROUND: How to minimize postoperative pain following spinal surgery has been a great challenge. We hypothesized that topical nonsteroidal anti-inflammatory drugs (NSAIDs) around the incision could relieve postoperative pain following transforaminal lumbar interbody fusion (TLIF) surgery. OBJECTIVE: This study tested the effect of topical NSAIDs around the incision for pain management after TLIF surgery. STUDY DESIGN: A double-blind randomized controlled trial. SETTING: Qilu Hospital of Shandong University. METHODS: Eighty patients who underwent single-level TLIF surgery were randomized into 2 groups. The treatment group received postoperative topical NSAIDs around the incision. The control group received a postoperative topical placebo around the incision. All patients in both groups received postoperative patient-controlled analgesia (PCA) via an analgesia pump. The primary outcome measures were the amount of opioid consumption and pain measurement via the visual analog scale (VAS). The secondary outcome measures were the time of first analgesic demand, operation time, postoperative drain output, side effects of opioids, postoperative stay, and Oswestry Disability Index (ODI) score. RESULTS: The consumption of opioids in the treatment group was significantly less than in the control group at postoperative 12 hours, 12 to 24 hours, and 24 to 48 hours (P < 0.005). The VAS in the treatment group was significantly lower than those in the control group at all assessment times within 72 hours postoperative (P < 0.005). The time of first analgesic demand of PCA in the treatment group was significantly longer than that in the control group (P < 0.005). The side effects of opioids were significantly less in the treatment group than in the control group (P < 0.05). There was no significant difference in operation time, postoperative drain output, postoperative stay, and ODI between the 2 groups (P > 0.05). LIMITATIONS: This was a single-center study for single-level TLIF surgery. CONCLUSION: Postoperative topical NSAID around the incision is a highly effective and safe method for postoperative pain management following single-level TLIF surgery. In our study it reduced postoperative opioid requirements and prolonged the time of first analgesic demand with no increased side effects. KEY WORDS: Transforaminal lumbar interbody fusion, postoperative pain, NSAID, topical NSAID, nonsteroidal anti-inflammatory drug, loxoprofen