Search

This study employed computational modeling (in silico) methods, combined with ecotoxicological experiments (in vivo) to predict the persistence/biodegradability, bioaccumulation, mobility, and ecological risks of an antihistamine drug (Loratadine: LOR) in the aquatic compartment. To achieve these goals, four endpoints of the LOR were obtained from different open-source computational tools, namely: (i) "STP total removal"; (ii) Predicted ready biodegradability; (iii) Octanol-water partition coefficient (KOW); and (iv) Soil organic adsorption coefficient (KOC). Moreover, acute and chronic, ecotoxicological assays using non-target freshwater organisms of different trophic levels (namely, algae Pseudokirchneriella subcapitata; microcrustaceans Daphnia similis and Ceriodaphnia dubia; and fish Danio rerio), were used to predict the ecological risks of LOR. The main results showed that LOR: (i) is considered persistent (after a weight-of-evidence assessment) and highly resistant to biodegradation; (ii) is hydrophobic (LOG KOW = 5.20), immobile (LOG KOC = 5.63), and thus, it can potentially bioaccumulate and/or can cause numerous deleterious effects in aquatic species; and (iii) after ecotoxicological evaluation is considered "toxic" and/or "highly toxic" to the three trophic levels tested. Moreover, both the ecotoxicological assays and risk assessment (RQ), showed that LOR is more harmful for the crustaceans (RQcrustaceans = moderate to high risks) than for algae and fish. Ultimately, this study reinforces the ecological concern due to the indiscriminate disposal of this antihistamine drug in worldwide aquatic ecosystems. [ABSTRACT FROM AUTHOR]

In order to improve the sensitivity of the newly established methodology, a thorough examination was carried out on the essential parameter. A rapid and highly responsive technique has been developed for the detection of loratadine. This method involves the generation of pale white species through the reaction between sodium nitroprusside and loratadine. The transducer's energy response was evaluated using the NAG-4SX3-3D analyzer. The linear range for measuring loratadine is 0.01-10 mM (millimolary). For concentrations of 4 and 10 mM. The RSD (relative standard deviation) for six trials was significantly lower than 0.14 percent. The measurement of loratadine has a limit of detection (LOD) of 261.890 ng/sample for (n=13). The calibration graph shows a progressive dilution across the lowest concentration linear dynamic range, with a correlation coefficient (r) of 0.9984. The percentage linearity (R2 %) is 99.68. The proposed approach was evaluated in comparison to the previous technique, which involved UV-spectrophotometric analysis at a wavelength of 275 nm. Based on the findings, it can be inferred that the technique exhibits enhanced sensitivity and surpasses the classic reference method's 10 mm irradiation, owing to its utilization of specific chemicals. Based on the aforementioned information, it is determined that the developed methodology is the most appropriate for analyzing loratadine in pharmaceutical samples when compared to the reference techniques.

Lysosomes are pivotal in cellular functions and disease, influencing cancer progression and therapy resistance with Acid Sphingomyelinase (ASM) governing their membrane integrity. Moreover, cation amphiphilic drugs (CADs) are known as ASM inhibitors and have anti-cancer activity, but the structural mechanisms of their interactions with the lysosomal membrane and ASM are poorly explored. Our study, leveraging all-atom explicit solvent molecular dynamics simulations, delves into the interaction of glycosylated ASM with the lysosomal membrane and the effects of CAD representatives, i.e., ebastine, hydroxyebastine and loratadine, on the membrane and ASM. Our results confirm the ASM association to the membrane through the saposin domain, previously only shown with coarse-grained models. Furthermore, we elucidated the role of specific residues and ASM-induced membrane curvature in lipid recruitment and orientation. CADs also interfere with the association of ASM with the membrane at the level of a loop in the catalytic domain engaging in membrane interactions. Our computational approach, applicable to various CADs or membrane compositions, provides insights into ASM and CAD interaction with the membrane, offering a valuable tool for future studies.

Objective(s): Ulcerative colitis is a chronic inflammatory bowel disease (IBD) that causes inflammation and ulcers in the rectum and the innermost layer of the large intestine. Our study aimed to elucidate the ameliorative effect of cetirizine (CTZ) and loratadine (LOR) against acetic acid-induced ulcerative colitis in rats via assessment of the PI3K/p-Akt/Nrf2 signaling pathway and proinflammatory cytokine release.Materials and Methods: Thirty-two rats were allocated into four groups (n=8). Group (I) was considered normal control. Acetic acid (AA) was injected intrarectally in groups (2-4). Group (2) was kept untreated. Group (3) was administered CTZ (20 mg/kg/day) for 7 days. Group (4) was administered LOR (10 mg/kg/day) for 7 days.Results: AA showed severe macroscopic colonic lesions associated with increased ulcer number, area, and severity with significantly elevated PI3K, p-Akt, Nrf2, TNF-α, and IL-6 in colorectal tissue as compared to the normal control group. All the aforementioned indicators were greatly improved by CTZ and LOR therapy.Conclusion: This is the first study to elucidate the ameliorative effect of CTZ and LOR against AA-induced UC in rats. CTZ and LOR treatment mitigates UC via amelioration of the PI3K/p-Akt/Nrf2 pathway and proinflammatory cytokine release.

Loratadine is metabolized to desloratadine. Both of them have been used for allergy treatment in children. Anatomical, physiological, and biological parameters of children and clearance of drugs vary with age. We aimed to develop a whole‐body physiologically based pharmacokinetic (PBPK) model to simultaneously predict the pharmacokinetics of loratadine and desloratadine in children. Following validation using 11 adult data sets, the developed PBPK model was extrapolated to children. Plasma concentrations following oral loratadine or desloratadine to children of different ages were simulated and compared with six children data sets. After scaling anatomy/physiology, protein binding, and clearance, pharmacokinetics of the two drugs in pediatric populations were satisfactorily predicted. Most of the observed concentrations fell within the 5th‐95th percentile range of the simulations in 1000 virtual children. The predicted area under the concentration‐time curve (AUC) and Cmax fell within 0.5‐2.0‐fold range of the observations. Oral doses of loratadine or desloratadine for children of different ages were simulated based on similar AUCs following 10 mg of loratadine or 5 mg of desloratadine for adults. Pediatric PBPK model was successfully developed to simultaneously predict plasma concentrations of loratadine and desloratadine in children of all ages. The developed pediatric PBPK model may also be applied to optimize pediatric dosage. [ABSTRACT FROM AUTHOR]

Objectives: Perennial allergic rhinitis (PAR) is common in Japan. Second-generation antihistamines (SGAs) are commonly used for its treatment; however, it remains unclear which SGA is the most cost-effective. Additionally, the pharmacoeconomics of Japanese Kampo shoseiryuto (which was traditionally prescribed to treat PAR in Japan) remains poorly understood. In this study, we aimed to investigate the effectiveness of various SGAs and shoseiryuto for the treatment of PAR in Japanese outpatients, from the healthcare payer's perspective. Methods: The most cost- and clinically effective SGAs were determined from a list of 6 SGAs (bepotastine, 10 mg; cetirizine, 10 mg; ebastine, 10 mg; epinastine, 20 mg; loratadine, 10 mg; and olopatadine, 5 mg) together with shoseiryuto, using the overall improvement rate through a model-based analysis. The time horizon was 28 days. Costs were determined based on the Medical Fee Index in 2020. Deterministic and probabilistic sensitivity analyses were conducted to address the uncertainty of the base-case results. Results: Overall, bepotastine (10 mg) and ebastine (10 mg) were cost-effective. Shoseiryuto was less cost-effective than ebastine (10 mg) (dominated). Ebastine (10 mg) was the most cost-effective option based on deterministic and probabilistic sensitivity analyses. Conclusions: Ebastine (10 mg) was the most cost-effective treatment strategy for PAR among the agents evaluated in this study. This insight could aid in establishing an appropriate formulary for treating PAR in hospitals and communities. [ABSTRACT FROM AUTHOR]

Seasonal allergies have a negative impact on patients' quality of life. Nurses must be aware of the different treatment options and lifestyle modifications to help patients manage their symptoms. This article discusses the benefits and risks of over-the-counter medications for seasonal allergies and other implications for nurses. [ABSTRACT FROM AUTHOR]

AbstractObjectiveMethodsTo investigate the clinical efficacy and safety of Loratadine combined with Glucocorticoid nasal spray in the treatment of pediatric bronchial asthma with seasonal allergic rhinitis.A total of 100 pediatric patients with moderate to severe bronchial asthma and seasonal allergic rhinitis admitted to our hospital between January 2020 and January 2023 were included in this study. All patients met the complete inclusion and exclusion criteria. Based on different treatment interventions, they were divided into the control group (n = 50) and the observation group (n = 50). Patients in the control group received treatment with glucocorticoid nasal spray, while patients in the observation group received combined intervention with Loratadine in addition to the treatment received by the control group. The clinical treatment outcomes, incidence of adverse reactions, as well as the scores of nasal symptoms, asthma control, and peak expiratory flow rates at different treatment time points (baseline, T1: 30 days after treatment, T2: 60 days after treatment, T3: 90 days after treatment) were compared between the two groups. The combined treatment of Loratadine with Glucocorticoid nasal spray demonstrates significant clinical efficacy in the treatment of pediatric bronchial asthma with seasonal allergic rhinitis. It further promotes the recovery of peak expiratory flow rates, improves symptoms of rhinitis and asthma in pediatric patients. Importantly, the application of this combined treatment does not increase the risk of adverse reactions in pediatric patients, indicating its high safety profile. This treatment approach is worthy of clinical application and further promotion. [ABSTRACT FROM AUTHOR]

Background: Granulocyte-colony stimulating factors (G-CSFs) are administered to many pediatric patients undergoing myelosuppressive cancer treatment to prevent febrile neutropenia. The most common side effect of G-CSF administration is bone pain, which can be debilitating and result in treatment delays and complications. The use of loratadine to safely and effectively manage G-CSF-induced bone pain in this population is examined. Methods: A literature review was performed using PubMed to locate relevant articles. Search terms included histamine antagonists, loratadine, granulocyte-colony stimulating factor, G-CSF bone pain, pegfilgrastim, and cancer-related bone pain. Ultimately, 18 peer-reviewed articles are included in this narrative review. Results: Current treatment options to manage bone pain are largely reliant on acetaminophen, nonsteroidal anti-inflammatory drugs, and opioids, but are not always feasible or effective. More recently, loratadine has been studied for its use in treating G-CSF-induced bone pain. As a second-generation antihistamine, loratadine is non-sedating and has shown to be beneficial in treating bone pain with minimal side effects. Conclusions: There appears to be benefit in the use of loratadine to treat bone pain with minimal risk. Although loratadine has been used extensively to treat bone pain caused by G-CSF in the adult population, more research is needed specifically in the pediatric setting. Evidence also suggests that loratadine may prove beneficial in treating other types of cancer-related bone pain as well, but more research is needed before making evidence-based practice recommendations. [ABSTRACT FROM AUTHOR]

Objective(s): Ulcerative colitis is a chronic inflammatory bowel disease (IBD) that causes inflammation and ulcers in the rectum and the innermost layer of the large intestine. Our study aimed to elucidate the ameliorative effect of cetirizine (CTZ) and loratadine (LOR) against acetic acid-induced ulcerative colitis in rats via assessment of the PI3K/p-Akt/Nrf2 signaling pathway and proinflammatory cytokine release. Materials and Methods: Thirty-two rats were allocated into four groups (n=8). Group (I) was considered normal control. Acetic acid (AA) was injected intrarectally in groups (2-4). Group (2) was kept untreated. Group (3) was administered CTZ (20 mg/kg/day) for 7 days. Group (4) was administered LOR (10 mg/kg/day) for 7 days. Results: AA showed severe macroscopic colonic lesions associated with increased ulcer number, area, and severity with significantly elevated PI3K, p-Akt, Nrf2, TNF-a, and IL-6 in colorectal tissue as compared to the normal control group. All the aforementioned indicators were greatly improved by CTZ and LOR therapy. Conclusion: This is the first study to elucidate the ameliorative effect of CTZ and LOR against AAinduced UC in rats. CTZ and LOR treatment mitigates UC via amelioration of the PI3K/p-Akt/Nrf2 pathway and proinflammatory cytokine release. [ABSTRACT FROM AUTHOR]

Background: This study was to develop loratadine (LTD) emulgels to treat localized skin allergy. Method: Initially oil-in-water emulsion was prepared by 3 different types of surfactants & finally gelling agent carbopol 940 was incorporated into emulsion to produce emulgel (i.e., standard conventional method). Results: The developed formulations were characterized using various parameters including particle size (PS), zeta potential (ZP), polydispersity index (PDI), entrapment efficacy (EE), pH, extrusion efficacy, physical stability, in-vitro drug release studies, and scanning electron microscopy (SEM). PS, EE, PDI, ZP and In-vitro studies ranges between 186.25 ± 6.42 mm (LE-F4) to 395.24 ± 8.64 mm (LE-F1), 62.38 ± 0.36 % (LE-F2) to 76.48 ± 0.69 % (LE-F4), 0.276 ± 0.02 (LE-F4) to 0.652 ± 0.02 (LE-F1), 16.45 ± 2.13 mV (LE-F1) to 29.46 ± 2.78 mV (LE-F3) and 21.90 ± 0.3 % (LE-F1) to 68.30±0.9 % (LE-F4) respectively. Conclusion: Based on all physicochemical properties, LE-F4 formulation was considered to be optimized with minimum PS (186.25±6.42 nm), PDI (0.276±0.02), satisfactory positive surface charge (23.15 ± 1.89 mV) and maximum EE (76.48±0.69 %). FTIR studies were confirmed that there is no physical interaction between drug and excipients and SEM studies revealed that vesicle size was spherical with smooth texture. A significantly greater rate of drug release (i.e., 68.30 ± 0.90%) was seen in the LTD emulgels that were made with cationic surfactant (i.e., LE-F4) and found to be good spreadability and extrudability.

Abstract Loratadine (LoR) is a highly lipophilic and practically insoluble in water, hence having a low oral bioavailability. As it is formulated as topical gel, it competitively binds with the receptors, thus reducing the side-effects. The objective of this study was to prepare LoR loaded nanosponge (LoR-NS) in gel for topical delivery. Nine different formulations of emulsion were prepared by solvent evaporation method with polyvinyl alcohol (PVA), ethyl cellulose (EC), and dichloromethane (DCM). Based on 32 Full Factorial Design (FFD), optimization was carried out by varying the concentration of LOR:EC ratio and stirring rate. The preparations were subjected for the evaluation of particle size (PS), in vitro release, zeta potential (ZP) and entrapment efficiency (EE). The results revealed that the NS dispersion was nanosized with sustained release profiles and significant PS. The optimised formulation was formulated and incorporated into carbopol 934P hydrogel. The formulation was then examined to surface morphological characterizations using scanning electron microscopy (SEM) which depicted spherical NS. Stability studies, undertaken for 2 months at 40 ± 2 °C/75 ± 5% RH, concluded to the stability of the formulation. The formulation did not cause skin irritation. Therefore, the prepared NS hydrogel proved to be a promising applicant for LoR as a novel drug delivery system (NDDS) for safe, sustained and controlled topical application.

Rapidly dissolving polymer thin films, or oral thin films (OTFs), have recently emerged as an improved oral drug delivery vehicle with its ability to bypass liver first pass metabolism, longer shelf-life, and simpler transport and distribution requirements, compared to traditional tablets and liquid formulations. Loratadine (LOR), an antihistamine commonly used to treat allergic rhinitis, undergoes liver first pass metabolism and is a prime candidate for incorporation within an OTF. However, loratadine is a BCS II drug with low aqueous solubility. Herein, the solubility of loratadine was improved by complexation with methyl β-cyclodextrin (MBCD) by co-evaporation of 2:1, 1:1, and 1:2 LOR:MBCD ratios and incorporation into a pullulan-based OTF at 4 wt% by solvent casting at 50 °C for 30 – 35 min. A therapeutically relevant 10 mg LOR dose could be prepared in a 3 cm by 3 cm OTF. The feasibility of complexation was observed with a B s -type phase solubility diagram, and complexation itself was confirmed via differential scanning calorimetry (DSC) by disappearance of the LOR melting peak, Fourier-transform infrared spectroscopy (FTIR) by shifting of the C=O peak, via 1H NMR spectroscopy by downfield shifting and change in peak multiplicity of the LOR aromatic protons, and via diffusion-ordered spectroscopy by a decrease in the diffusion coefficient of LOR:MBCD complex. LOR:MBCD could be incorporated homogeneously throughout an OTF, and LOR:MBCD OTFs exhibited reasonable mechanical strength and endured 12 ± 3 folds before breaking. LOR:MBCD OTFs disintegrated within 38 ± 10 s. The cumulative in vitro release of LOR:MBCD OTFs peaked at 80 % within 3–4 min of dissolution, and LOR in LOR:MBCD OTFs exhibited permeability across a 0.22 μm nitrocellulose membrane, demonstrating its applicability as a rapid drug delivery vehicle. [Display omitted] [ABSTRACT FROM AUTHOR]

Neurological injury is a crucial problem that interferes with the therapeutic use of vinca alkaloids as well as the quality of patient life. This study was conducted to assess the impact of using loratadine or diosmin/hesperidin on neuropathy induced by vinca alkaloids. Patients were randomized into one of three groups as follows: group 1 was the control group, group 2 received 450 mg diosmin and 50 mg hesperidin combination orally twice daily, and group 3 received loratadine 10 mg orally once daily. Subjective scores (numeric pain rating scale, douleur neuropathique 4, and functional assessment of cancer therapy/gynecologic oncology group–neurotoxicity (FACT/GOG-Ntx) scores), neuroinflammation biomarkers, adverse drug effects, quality of life, and response to chemotherapy were compared among the three groups. Both diosmin/hesperidin and loratadine improved the results of the neurotoxicity subscale in the FACT/GOG-Ntx score (p < 0.001, p < 0.01 respectively) and ameliorated the upsurge in neuroinflammation serum biomarkers. They also reduced the incidence and timing of paresthesia (p = 0.001 and p < 0.001, respectively) and dysuria occurrence (p = 0.042). Both loratadine and diosmin/hesperidin attenuated the intensity of acute neuropathy triggered by vinca alkaloids. Furthermore, they did not increase the frequency of adverse effects or interfere with the treatment response. [ABSTRACT FROM AUTHOR]

To gain a comprehensive overview of the landscape of clinical trials for the H1-receptor antagonists (H1R antagonists) cetirizine, levocetirizine, loratadine, desloratadine, and fexofenadine and their potential use cases in drug repurposing (the use of well-known drugs outside the scope of the original medical indication), we analyzed trials from clincialtrials.gov using novel custom-coded software, which itself is also a key emphasis of this paper. To automate data acquisition from clincialtrials.gov via its API, data processing, and storage, we created custom software by leveraging a variety of open-source tools. Data were stored in a relational database and annotated facilitating a specially adapted web application. Through the data analysis, we identified use cases for repurposing and reviewed backgrounds and results in the scientific literature. Even though we found very few trials with published results for repurpose indications, extended literature research revealed some prominent use cases: Cetirizine seems promising in mitigating infusion-associated reactions and is also more effective than placebo in the treatment of androgenetic alopecia. Loratadine may be beneficial in the prophylaxis of G-CSF-related bone pain. In COVID-19, H1R antagonists may be helpful, but placebo-controlled scientific evidence is needed. For asthma, the effect of H1R antagonists only seems to be secondary by alleviating allergy symptoms. Our novel method to find potential use cases for repurposing of H1R antagonists allows for high automation, reduces human error, and was successful in revealing potential areas of interest. The software could be used for similar research questions and analyses in the future. [ABSTRACT FROM AUTHOR]

Loratadine (LoR) is a highly lipophilic and practically insoluble in water, hence having a low oral bioavailability. As it is formulated as topical gel, it competitively binds with the receptors, thus reducing the side-effects. The objective of this study was to prepare LoR loaded nanosponge (LoR-NS) in gel for topical delivery. Nine different formulations of emulsion were prepared by solvent evaporation method with polyvinyl alcohol (PVA), ethyl cellulose (EC), and dichloromethane (DCM). Based on 32 Full Factorial Design (FFD), optimization was carried out by varying the concentration of LOR:EC ratio and stirring rate. The preparations were subjected for the evaluation of particle size (PS), in vitro release, zeta potential (ZP) and entrapment efficiency (EE). The results revealed that the NS dispersion was nanosized with sustained release profiles and significant PS. The optimised formulation was formulated and incorporated into carbopol 934P hydrogel. The formulation was then examined to surface morphological characterizations using scanning electron microscopy (SEM) which depicted spherical NS. Stability studies, undertaken for 2 months at 40 ± 2 °C/75 ± 5% RH, concluded to the stability of the formulation. The formulation did not cause skin irritation. Therefore, the prepared NS hydrogel proved to be a promising applicant for LoR as a novel drug delivery system (NDDS) for safe, sustained and controlled topical application. [ABSTRACT FROM AUTHOR]

Second-generation tricyclic H1 antihistamine loratadine (LTD) has a high permeability, low water solubility, and an oral absorption rate dependent on the rate at which it dissolves in the gastrointestinal tract. One approach suggested for improving the drug's solubility and rate of dissolution is natural solid dispersion (NSD). The present study evaluated the use of hydrophilic natural polymers, sodium alginate (SA), hyaluronic acid (HA), and xyloglucan (XG), in natural solid dispersion to enhance LTD solubility and dissolution rate. A total of 12 formulations comprising varied drug-to-polymer ratios were produced and analyzed for percentage yield, water solubility, and in vitro dissolution rate. The solubility of LTD was improved in all formulations. Excellent results were achieved with NSD1 (LTD: SA 1:0.25), with a high yield (99%), superior solubility (0.187) compared to pure loratadine (0.0021), and a speedy dissolution rate (98%) within 30 minutes. These studies suggest natural polymers like SA, HA, and XG can considerably increase LTD solubility. When introduced into NSD, these polymers effectively augment LTD dissolving rates, presenting attractive prospects for better bioavailability and therapeutic efficacy. [ABSTRACT FROM AUTHOR]

Abstract Background Tumor-associated inflammation suggests that anti-inflammatory medication could be beneficial in cancer therapy. Loratadine, an antihistamine, has demonstrated improved survival in certain cancers. However, the anticancer mechanisms of loratadine in lung cancer remain unclear. Objective This study investigates the anticancer mechanisms of loratadine in lung cancer. Methods A retrospective cohort of 4,522 lung cancer patients from 2006 to 2018 was analyzed to identify noncancer drug exposures associated with prognosis. Cellular experiments, animal models, and RNA-seq data analysis were employed to validate the findings and explore the antitumor effects of loratadine. Results This retrospective study revealed a positive association between loratadine administration and ameliorated survival outcomes in lung cancer patients, exhibiting dose dependency. Rigorous in vitro and in vivo assays demonstrated that apoptosis induction and epithelial-mesenchymal transition (EMT) reduction were stimulated by moderate loratadine concentrations, whereas pyroptosis was triggered by elevated dosages. Intriguingly, loratadine was found to augment PPARγ levels, which acted as a gasdermin D transcription promoter and caspase-8 activation enhancer. Consequently, loratadine might incite a sophisticated interplay between apoptosis and pyroptosis, facilitated by the pivotal role of caspase-8. Conclusion Loratadine use is linked to enhanced survival in lung cancer patients, potentially due to its role in modulating the interplay between apoptosis and pyroptosis via caspase-8.

Background: Tumor-associated inflammation suggests that anti-inflammatory medication could be beneficial in cancer therapy. Loratadine, an antihistamine, has demonstrated improved survival in certain cancers. However, the anticancer mechanisms of loratadine in lung cancer remain unclear. Objective: This study investigates the anticancer mechanisms of loratadine in lung cancer. Methods: A retrospective cohort of 4,522 lung cancer patients from 2006 to 2018 was analyzed to identify noncancer drug exposures associated with prognosis. Cellular experiments, animal models, and RNA-seq data analysis were employed to validate the findings and explore the antitumor effects of loratadine. Results: This retrospective study revealed a positive association between loratadine administration and ameliorated survival outcomes in lung cancer patients, exhibiting dose dependency. Rigorous in vitro and in vivo assays demonstrated that apoptosis induction and epithelial-mesenchymal transition (EMT) reduction were stimulated by moderate loratadine concentrations, whereas pyroptosis was triggered by elevated dosages. Intriguingly, loratadine was found to augment PPARγ levels, which acted as a gasdermin D transcription promoter and caspase-8 activation enhancer. Consequently, loratadine might incite a sophisticated interplay between apoptosis and pyroptosis, facilitated by the pivotal role of caspase-8. Conclusion: Loratadine use is linked to enhanced survival in lung cancer patients, potentially due to its role in modulating the interplay between apoptosis and pyroptosis via caspase-8. [ABSTRACT FROM AUTHOR]

Background: The work aimed to fabricate Loratadine (LRD) niosomes by employing a Box Behnken Design (BBD) and they were subsequently applied to transdermal patches utilizing BBD's solvent casting process. Materials and Methods: The prepared niosomes were assessed for their size, shape, zeta potential, and level of entrapment efficiency. The niosomal formulations that have been optimized were inserted into a patch system. Then, physico-chemical characteristics, and in vitro permeation studies were used to characterize each patch. Results: In comparison patches loaded with niosomal vesicles showed better drug release compared to the control patches. Niosomal patches had higher permeation than control patches, it was discovered. The surfactant in niosomes acts as a penetration enhancer, which helps to improve LRD permeation from niosomes. Conclusion: The work summarizes that the transdermal patches based on niosomes could efficiently deliver LRD medicines trans-dermally while preventing GIT side effects. [ABSTRACT FROM AUTHOR]

Loratadine, a BCS class II drug, is used as an antihistaminic in the treatment of allergies. It has a poor water solubility and a low bioavailability as a result of significant first-pass hepatic metabolism after oral administration. Nanofibers, which are strings of polymeric fibres with diameters smaller than 1 micron, are one such strategy. They are superior to other varieties of the substance in a number of ways, including surface area to volume ratio, elasticity, and mechanical properties. Typically, electrospinning is used to make nanofibers. These properties could be utilized for overcoming the problems associated with the loratadine. Thus, the aim of this study was to formulate loratadine nanofiber film for buccal application. The formulation of loratadine nanofiber films involved electrospinning a solution containing a definite ratio of Polyvinylpyrrolidone (PVP) and Ethyl Cellulose (EC). The optimized film was characterized by SEM, DSC and FTIR. Mucoadhesion strength, ex-vivo permeation tests, and invitro drug release were all assessed for the end formulation. The results showed that the drug was evenly dispersed and enclosed within the nanofiber matrix. The film made of nanofibers showed consistent morphology and enhanced drug penetration and release. The developed Loratadine-loaded electrospun nanofiber film may therefore be used as an improvement over conventional dosage forms by increasing patient compliance. [ABSTRACT FROM AUTHOR]

Histamine receptors play a pivotal role in various physiological functions (ranging from allergic responses to memory and sleep regulation), hence representing important drug targets. While second-generation antihistamines have successfully been used in rodents and humans, testing their effects in non-traditional animal models furthers our understanding of their physiological activity and facilitates the development of novel drug candidates. Here, we examined the effects of the first-generation antihistaminic drug chloropyramine and the second-generation drugs loratadine and cetirizine, at concentrations of 1, 5, and 10 mg/L, on adult zebrafish behavior in the novel tank test. All three drugs significantly altered zebrafish locomotor activity, decreasing the distance traveled and average velocity, as well as increasing low acceleration frequency. Chloropyramine (5 and 10 mg/L) and loratadine (1, 5, and 10 mg/L) also significantly reduced top entries compared to the control. Additionally, chloropyramine (5 mg/L) increased the total duration of top entries, whereas loratadine (10 mg/L) reduced this behavior compared to controls. Overall, chloropyramine and loratadine exhibited a sedative effect typical of antihistamines, whereas cetirizine solely reduced locomotor activity without affecting other patterns of fish behavior. Thus, cetirizine demonstrated the least side effects on the central nervous system among the studied drugs, making it the optimal and safest choice among antihistamines. [ABSTRACT FROM AUTHOR]

Recently, the aim of analytical community is to reduce the usage of hazardous chemicals; so eco-friendly, rapid, selective and cost-effective methods were developed for simultaneous determination of montelukast sodium (MKT) and loratadine (LRT). The first method was based on chromatographic separation performed on precoated silica gel 60 GF254 plates with ethyl acetate–ethanol 9: 1 (v/v) as the mobile phase. The developed plates were scanned and quantified at 260 nm. The method gives linear correlation over concentration ranges of 0.3–3.6 μg/spot and 0.2–4.0 μg/spot for MKT and LRT, respectively. It was also successfully applied to analysis of both drugs in their pharmaceutical preparation and human plasma. The other methods are UV-spectrophotometric methods based on smart spectra manipulating to zero order spectrum of each drug. These methods are named response correlation (RC), a-centering and ratio derivative methods. RC and a-centering methods were dependent on the presence of an isosbestic point between the overlapped spectra of both drugs. While ratio derivative method based on manipulation of the ratio spectra of both drugs. The two drugs obey Beer–Lambert law over the concentration ranges of 3.0–30.0 μg/mL in the three spectrophotometric methods. Moreover, the greenness of the developed methods is assessed using suitable analytical Eco-Scale and Green Analytical Procedure Index. [ABSTRACT FROM AUTHOR]

Loratadine (LRD), a non-sedating and slow-acting antihistamine, is often given in combination with short-onset chlorpheniramine maleate (CPM) to increase efficacy. However, LRD has poor water solubility resulting in low bioavailability. The aim of this study was to improve LRD solubility by preparing co-amorphous LRD-CPM. However, the obtained co-amorphous LRD-CPM recrystallized rapidly, and the solubility of LRD returned to a poor state again. Therefore, co-amorphous LRD-CPM solid dispersions using polyvinylpyrrolidone (PVP) as a carrier were prepared. The obtained solid dispersions were characterized using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR). The solubility, dissolution, and mechanism of drug release from the LRD-CPM/PVP co-amorphous solid dispersions were studied and compared with those of intact LRD, LRD/PVP solid dispersions, and co-amorphous LRD-CPM mixtures. The results from XRPD and DSC confirmed the amorphous form of LRD in the co-amorphous solid dispersions. The FTIR results indicated that there was no intermolecular interaction between LRD, CPM, and PVP. In conclusion, the obtained LRD-CPM/PVP co-amorphous solid dispersions can successfully increase the water solubility and dissolution of LRD and extend the amorphous state of LRD without recrystallization. [ABSTRACT FROM AUTHOR]

Pollen-food allergy syndrome (PFAS) is a common IgE-mediated allergic condition resulting from cross-reactions between pollen and plant food allergens, primarily those in the PR-10 subfamily. Mostly symptoms are limited to the mouth and throat causing oral allergy syndrome (OAS). Systemic reactions are extremely rare. We report an 11-year-old boy who experienced a unique anaphylactic reaction after consuming raw carrot juice. The patient exhibited symptoms within one minute, including abdominal pain, facial and eyelid swelling, dyspnea, a macular rash, choking sensation and drowsiness. Desloratadine alleviated these symptoms, and as his overall condition improved rapidly, there was no need for adrenaline administration. Carrot-specific IgE levels in the patient's serum were as follows: Dau c: 40.63 kUA/L and Dau c1: 31.5 kUA/L. He had previously been diagnosed with seasonal allergic rhinoconjunctivitis. The high degree of similarity among allergen components within the PR-10 subfamily contributed to cross-reactivity between birch pollen and carrots. It is important to remember that PFAS can manifest systemically, with symptoms ranging from mild skin itching to potentially fatal consequences. This highlights the need for healthcare professionals to be extra cautious and aware of this possibility, especially since carrots are commonly found in a wide range of dishes and snacks. [ABSTRACT FROM AUTHOR]

Background: Loratadine and montelukast are clinical first-line drugs in the treatment of allergic rhinitis (AR). However, there is no clear evidence of the efficacy of loratadine combined with montelukast in the treatment of AR. This study aimed to evaluate the efficacy and safety of the loratadine-montelukast combination on AR. Methods: In this meta-analysis, searches were conducted on PubMed, Embase, the Cochrane Central Register of Controlled Trials, Web of Science, and China National Knowledge Infrastructure (CNKI). The search terms included loratadine, montelukast, allergic rhinitis, and clinical trials. Meta-analyses were conducted using Rev Man 5.3 and Stata 15 statistical software. Results: A total of 23 studies with 4,902 participants were enrolled. For the primary outcome, pooled results showed that loratadine-montelukast can significantly reduce total nasal symptom scores (TNSS), when compared with loratadine (SMD, -1.00; 95% CI, -1.35 to -0.65, p < 0.00001), montelukast (SMD, -0.46; 95% CI, -0.68 to -0.25, p < 0.0001), or placebo (SMD, -0.93; 95% CI, -1.37 to -0.49, p < 0.00001). For secondary outcomes, pooled results showed that compared with loratadine, loratadine-montelukast can significantly improve nasal congestion, nasal itching, nasal sneezing, nasal rhinorrhea, and rhinoconjunctivitis quality of life questionnaires (RQLQ). Compared with montelukast, loratadine-montelukast can significantly improve nasal itching, and nasal sneezing. Compared with placebo, loratadine-montelukast can significantly improve nasal congestion, and RQLQ. Conclusion: Loratadine-montelukast combination is superior to loratadine monotherapy, montelukast monotherapy, or placebo in improving AR symptoms. Therefore, loratadine-montelukast combination can be an option for patients with moderate-severe AR or poorly response to monotherapy. Systematic review registration number: clinicaltrials.gov, identifier CRD42023397519. [ABSTRACT FROM AUTHOR]