Olopatadine Research Articles

Implantation of impressive chromatographic and built-in UV spectrophotometry approaches for sustainable Estimation of olopatadine and mometasone in pharmaceuticals; eco-scale and BAGI applications

The development of analytical methods that adhere to the principles of sustainable green chemistry is essential in the modern scientific arena. This research presents two novel methods for the concurrent quantification of olopatadine (OLO) and mometasone (MOM), targeting sustainable green chemistry principles in their raw materials, dosage forms and combined nasal spray formulations. The first method is a rapid isocratic high-performance liquid chromatography (HPLC) that achieves excellent resolution within 4 min, with retention times of 2.37 ± 0.1 min for OLO and 4.05 ± 0.1 min for MOM. It features optimal sensitivity, with detection limits of 0.13 µg/mL for OLO and 0.03 µg/mL for MOM. It utilizes a cyano column with an isocratic mobile phase of acetonitrile and 0.1 M OPA (50: 50, v/v), making it accessible to standard laboratory equipment. The second method is UV–visible spectrophotometry, which includes first-order derivative measurement (D1) and ratio derivative spectra (RDS) methods. These spectroscopic approaches provide linear response range of 0.2–20.0 µg/mL for OLO and 4.0–40.0 µg/mL for MOM, respectively serving as cost-effective alternatives for labs with limited resources. Validation results show high accuracy (98–102 %) and precision (RSD < 2 %). Green assessments using Eco-Scale indicate scores of 86 for HPLC and 100 for spectrophotometry, while the “blueness” concept via BAGI demonstrates strong sustainability with scores of 87.5 and 90. These methods effectively quantify OLO and MOM in their raw materials, different formulations and combined nasal spray, providing a sustainable and reliable approach for pharmaceutical analysis. This work is the first green assessment for the determination of OLO and MOM in pure drug and in the pharmaceutical formulations using less hazard solvent and simple technique.

A comparative study of efficacy and tolerability of bepotastine besilate (1.5%) and olopatadine hydrochloride (0.1%) eye drops in allergic conjunctivitis in a tertiary care hospital of the southern part of India

Background: Allergic conjunctivitis is increasing with the rise in the levels of allergens. Drug therapy is usually needed in addition to avoidance of general allergens to treat this condition. Both bepotastine besilate and olopatadine hydrochloride ophthalmic solutions are newer additions in the treatment of allergic conjunctivitis having dual properties of second-generation antihistaminics along with mast cell stabilizing activity. Aims and Objectives: The aim of the study was to compare the efficacy and tolerability of bepotastine besilate (1.5%) and olopatadine hydrochloride (0.1%) eye drops in patients presenting with allergic conjunctivitis in a tertiary care hospital of Southern part of India. Materials and Methods: Sixty patients who were clinically diagnosed to be suffering from allergic conjunctivitis were selected as participants for the study. They were randomly distributed into two groups consisting of 30 patients each. One group received eye drop bepotastine (1.5%) and the other group received eye drop olopatadine (0.1%), with each patient receiving the medication twice daily for a duration of 2 weeks. During the first visit, all the patients were assessed for the signs and symptoms and subsequently re-assessed at weekly intervals for a period of 2 weeks. They were also advised to report occurrence of any unwanted drug reaction during the weekly follow-up visits. Results: The above study showed the effectiveness of both bepotastine and olopatadine eye drops in decreasing the signs and symptoms of allergic conjunctivitis. Significant clinical improvement was found in all participants, whereas deterioration was found in none of them. Statistically significant improvement of itching and redness of eyes was observed with use of both the study drugs mentioned beforehand. Both the drugs were well tolerated by the patients. Statistically significant reduction of itching and foreign body sensation was found to be more in patients using bepotastine eye drops compared to those using olopatadine eye drops. Only two patients using bepotastine eye drops complained of having a mild burning sensation in eyes. Conclusion: From this study, bepotastine and olopatadine eye drops have been observed to be safe and efficacious in allergic conjunctivitis. Bepotastine eye drop was found to be more efficacious to relieve itching and foreign body sensation compared to that of olopatadine eye drops.

Development of a Temperature and pH Dual-Sensitive In-Situ Gel for Treating Allergic Conjunctivitis.

The purpose of this study was to improve the efficacy of olopatadine hydrochloride (OT) in treating allergic conjunctivitis (AC). To achieve this goal, we developed an eye formulation without antimicrobial agents using a temperature-pH dual-sensitive in situ gel technology combined with heat sterilization. Various types of carbomers were evaluated and their optimal doses determined. The prescription containing poloxamer 407 (P407) and poloxamer 188 (P188) was optimized using central composite design for response surface methodology (CCD-RSM). The final optimized dual-sensitive in situ gel (TP-gel) consisted of 0.1% olopatadine hydrochloride, 18.80% P407, 0.40% P188, 0.30% Pemulen™TR-1(TR-1), 4.0% mannitol, and 0.08% Tri(hydroxymethyl)aminomethane(Tris).Sterilization was performed at a temperature of 121℃ for a duration of 20 min. Experimental results showed that TP-gel had good safety profile and remained on the ocular surface for approximately (65.83 ± 8.79) minutes, which is four times longer than eye drops. The expression levels of IL-13, IL-17, and OVA-IgE in mouse ocular tissues with allergic conjunctivitis treated with TP-gel were significantly reduced. This suggests that TP-gel has the potential to be an effective treatment method for allergic conjunctivitis.

Food and bile micelle binding of zwitterionic antihistamine drugs.

The food effects on oral drug absorption are challenging to predict from in vitro data. Food intake has been reported to reduce the oral absorption of several zwitterionic antihistamine drugs. However, the mechanism for this negative food effect has not been clear. The purpose of the present study was to evaluate the bile micelle and food binding of zwitterionic antihistamine drugs as a possible mechanism for the negative food effects on their oral drug absorption. Bilastine (BIL), cetirizine (CET), fexofenadine (FEX), and olopatadine (OLO) were employed as model drugs. The fed/fasted AUC ratios of BIL, CET, FEX, and OLO after oral administration are reported to be 0.60 to 0.7, 0.92, 0.76 to 0.85, and 0.84, respectively. The unbound fraction (f u) of these drugs in the fasted and fed state simulated intestinal fluids (FaSSIF and FeSSIF, containing 3 and 15 mM taurocholic acid, respectively) with or without FDA breakfast homogenate (BFH) was measured by dynamic dialysis. The FeSSIF/ FaSSIF fu ratios were 0.90 (BIL), 0.46 (CET), 0.76 (FEX), and 0.78 (OLO). In the presence of BFH, the fu ratios were reduced to 0.52 (BIL), 0.22 (CET), 0.39 (FEX), and 0.44 (OLO). Despite being zwitterion at pH 6.5, the antihistamine drugs were bound to bile micelles. Bile micelle and food binding were suggested to cause a negative food effect on the oral absorption of these drugs. However, the AUC ratio was not quantitatively predicted by using FeSSIF + BFH.

Clinically Relevant Characterization and Comparison of Ryaltris and Other Anti-Allergic Nasal Sprays.

The deposition, residence time, and dissolution profile of nasal suspensions containing corticosteroids play a key role in their in vivo efficacy after administration. However, the conventional methods available to characterize nasal products appear to be unsuitable to exhaustively cover these aspects. The work aims to investigate technological aspects of Ryaltris (mometasone furoate and olopatadine hydrochloride nasal spray) compared to other commercial anti-allergic nasal products, namely, Dymista (azelastine hydrochloride and fluticasone propionate), Nasonex (mometasone furoate), and Avamys (fluticasone furoate). Innovative characterization methods were combined with more traditional approaches to investigate the anti-allergic nasal sprays. These methods applied together allowed to differentiate between the different products and provided a clear picture of the nasal product behavior in terms of drug dissolution and deposition. In particular, the dissolution tests were performed exploiting the Respicell® apparatus, an innovative technique that allows for the investigation of inhalation products. Then, formulation viscosities were considered along with a formulation flow test on an inclined plane. Finally, the intranasal deposition profile of the commercial formulations was determined using a silicon nasal cast. The results highlight in vitro significant differences in terms of viscosity as well as dissolution rate of the nasal products, with Ryaltris showing a higher viscosity and lower flow compared to other products, which, along with a corticosteroid faster dissolution rate than Dymista, suggest a potential advantage in terms of clinical behavior.

Green and sensitive detection of olopatadine in aqueous humor using a signal-on fluorimetric approach: GREEnness assessment.

Olopatadine (OLP) is widely utilized as an effective antihistaminic drug for alleviating ocular itching associated with allergic conjunctivitis. With its frequent usage in pharmacies, there arises a pressing need for a cost-effective, easily implementable, environmentally sustainable detection method with high sensitivity. This study presents a novel signal-on fluorimetric method for detecting OLP in both its pure form and aqueous humor. The proposed approach depends on enhancing the weak intrinsic fluorescence emission of OLP, achieving a remarkable increase of up to 680% compared to its intrinsic fluorescence. This enhancement is achieved by forming micelles around protonated OLP using an acetate buffer (pH 3.6) and incorporating a solution of sodium dodecyl sulfate (SDS) surfactant. A strong correlation (R = 0.9996) is observed between the concentration of OLP and fluorescence intensities ranging from 1.0 to 100.0 ng mL-1 with a limit of detection of 0.22 ng mL-1. This described method is successfully employed for quantifying OLP in both its powder form and pharmaceutical eye drops. Furthermore, it demonstrates robust performance in determining OLP in artificial aqueous humor with a percentage recovery of 99.05 ± 1.51, with minimal interference from matrix interferents. Moreover, the greenness of the described method was evaluated.

Erratum: Electro‐elucidation and quantification of olopatadine hydrochloride in bulk form and eye drops using modification free glassy carbon electrode with its development by different electrolytes and surfactants

Erratum: Electro‐elucidation and quantification of olopatadine hydrochloride in bulk form and eye drops using modification free glassy carbon electrode with its development by different electrolytes and surfactants

Simultaneous estimation of mometasone furoate and olopatadine hydrochloride by reversed‐phase high‐performance liquid chromatography

AbstractThe simultaneous determination of Mometasone furoate (MOM) and Olopatadine hydrochloride (OLO) in a combined dose has been developed and validated using a specific, precise, accurate, fast, reliable, and economical high‐performance liquid chromatography technique. Methanol:water:acetonitrile (20:25:55, v/v/v) was used as the mobile phase during the separation. The procedure was performed using a low‐pressure gradient elution on the reversed‐phase Phenomenex C18 column. At 238 nm, separated components were densitometrically measured. The flow rate was fixed at 1.0 mL/min with a continuous run up to 10 min, while the retention time was located near about 3.2 and 6.1 min for OLO and MOM, respectively. The method was validated for Linearity and range, precision, reproducibility, specificity, accuracy, limit of detection, limit of quantification, and robustness as per the International Council for Harmonization Q2(R1) guideline. MOM and OLO regression coefficients (r2) were found to be 0.9994 and 0.9997, over the range of 2.5–15 and 33.25–199.5 µg/mL, respectively. MOM and OLO percentage recoveries were measured to be 99.49 ± 0.14 and 99.98 ± 0.22, respectively. The method can be successfully applied for routine analysis of the quantitative determination of MOM and OLO in a combined dose.

Comparing the efficacy of Olopatadine Hydrochloride and Alcaftadine in the treatment of Allergic Conjunctivitis

Comparing the efficacy of Olopatadine Hydrochloride and Alcaftadine in the treatment of Allergic Conjunctivitis

Sustained Delivery of Olopatadine from Vitamin-E Loaded Contact Lenses.

Purpose: Topical antihistamines, such as olopatadine hydrochloride, an H1 receptor antagonist, are commonly prescribed for treating allergic conjunctivitis. Drug delivery via eye drops has many deficiencies including a short residence time due to tear drainage via the nasolacrimal duct, which results in a low bioavailability and potential for side effects. These deficiencies could be mitigated by a drug-eluting contact lens such as the recently approved ACUVUE® THERAVISION™ WITH KETOTIFEN which is a daily disposable etafilcon, a drug-eluting contact lens with ketotifen (19 μg per lens). Here, we investigate the feasibility of designing a drug-eluting lens with sustained release of olopatadine for treating allergies using an extended wear lens. Methods: Nanobarrier depots composed of vitamin-E (VE) are formed through direct entrapment by ethanol-driven swelling. The drug-loaded lenses are characterized for transparency and water content. In vitro release is measured under sink conditions and fitted to a diffusion control release model to determine diffusivity and partition coefficient. Results: In vitro studies indicate that ACUVUE OASYS® and ACUVUE TruEye™ lenses loaded with ∼0.3 g of VE/g of hydrogel effectively prolong olopatadine dynamics by 7-fold and 375-fold, respectively. Incorporation of VE into the lenses retains visible light transmission and other properties. Conclusion: The VE incorporation in commercial lenses significantly increases the release duration offering the possibility of antiallergy extended wear lenses.

NOVEL UV SPECTROPHOTOMETRIC METHOD FOR SIMULTANEOUS ESTIMATION OF MONTELUKAST SODIUM AND OLOPATADINE HYDROCHLORIDE USING ABSORBANCE CORRECTION PRINCIPLE

A simple, accurate and economical UV spectroscopic method has been developed for the simultaneous estimation of olopatadine hydrochloride and montelukast sodium. The developed method is based on the determination of the two drugs using UV absorbance correction principle. The wavelengths chosen for analysis were 352 nm for montelukast sodium (as absorbance due to the other drug was nil at this wavelength) and 298.5 nm for olopatadine hydrochloride (corrected for absorbance due to montelukast sodium) with water as diluent. The Beer-Lambert’s range for the two drugs was found to be 2-100 μg mL-1 at 298.5 nm and 2-70 μg mL-1 at 352 nm for montelukast sodium with r2 of ≥ 0.990. The developed method was validated as per ICH guidelines and the percentage assay results were within acceptable limits. The developed method can thus be successfully used for the regular analysis of olopatadine hydrochloride and montelukast sodium in bulk and in combination.

Determination of antihistaminic drugs alcaftadine and olopatadine hydrochloride via ion-pairing with eosin Y as a spectrofluorimetric and spectrophotometric probe: application to dosage forms

Four sensitive and fast analytical approaches relied on ion pairing with eosin Y were built up and evaluated using spectroscopy for determination of Alcaftadine and Olopatadine hydrochloride with high sensitivity and selectivity. Two spectrofluorimetric techniques were employed to observe the quenching effect of Alcaftadine or Olopatadine hydrochloride on the intrinsic fluorescence of eosin Y in a 0.1 M acetate buffer solution at pH 3.8 and 3.3 for Alcaftadine and Olopatadine hydrochloride, respectively. Those methods are considered the first spectrofluorimetric methods for Alcaftadine and Olopatadine hydrochloride assay. The fluorescence quenching effect was linear with concentration ranging from 150 to 2000 and 200 to 2000 ng mL−1 for Alcaftadine and Olopatadine hydrochloride, respectively. In the two spectrophotometric techniques, the absorbance of the produced ion-pair was monitored at 548 and 547 nm in aqueous buffered solution at pH 3.8 and 3.3 for Alcaftadine and Olopatadine hydrochloride, respectively. Beer's law was obeyed in the concentrations range of 0.8–8.0 and 1.0–10.0 µg mL−1. The four techniques were evaluated in accordance with ICH requirements and were effectively used to analyze dosage forms with a high percent recovery.

Ефективність та безпечність інтраназального застосування фіксованої комбінації олопатадину гідрохлориду та мометазону фуроату в терапії пацієнтів з алергічним ринітом

Abstract. One of the options for pharmacotherapy of allergic rhinitis (AR) with values of visual analogue assessment of symptoms ≥ 5 is the use of intranasal H1-histamine blocker in combination with intranasal cocorticosteroid. One of the new combinations that qualitatively corresponds to this composition is the combination of olopatadine hydrochloride and mometasone furoate. The aim of the study was to study the effectiveness and safety of symptomatic therapy by the fixed combination of olopatadine hydrochloride and mometasone furoate in the form of a nasal spray in the treatment of AR. Materials and methods. 45 patients were examined, of which 37 patients completed treatment (8 patients dropped out of the study due to poor compliance). All of them made up the main group of the study (age — 29.3 (16.6; 42.0) years, men — 13 (35.0 %), women — 24 (65.0 %). The design of the study was randomized prospective with interventional model in the form of monoprescription. The diagnosis of AR was established in accordance with the ARIA guidelines. To control nasal symptoms before and during treatment, a generally accepted scoring system was used — the TNSS scale (Total nasal symptom score), eye symptoms — the TOSS scale (Total ocular symptom score) The Rhinoconjunctivitis Quality of Life mini Questionnaire (RQLQ) was used to assess the quality of life of AR patients. The results. In the course of treatment, a statistically significant improvement in nasal symptoms (TNSS) was noted — a decrease in severity from 10.11 (8.71; 11.51) points to 1.31 (1.00; 1.63) points on the 28-th day of treatment (p &lt; 0.05). A similar statistically significant improvement was observed in the severity of ocular symptoms (TOSS) — a decrease in severity from 3.31 (1.81, 4.81) points to 0.36 (0.30, 0.42) points on the 28-th day of treatment (p &lt; 0.05). A statistically significant improvement in the quality of life according to the RQLQ during treatment was noted — the score decreased from 3.04 (2.72; 3.37) points at the initial visit to 1.83 (1.61; 2.05) points on the 7-th day. 1.02 (0.86, 1.18) points on day 14, 0.63 (0.51, 0.75) points on day 21 and 0.45 (0.41, 0.49) points on day 28 treatment (p &lt; 0.05). Conclusion. A fixed combination of mometasone furoate and olopatadine hydrochloride was effective in relieving nasal and ocular symptoms in patients with moderate/severe AR, reducing the TONSS score from 13.42 (10.81; 16.03) to 1.67 (1.14; 2.20) points and in improving the quality of life, reducing the degree of discomfort from 3.04 (2.72; 3.37) points to 0.45 (0.41; 0.49) points. For 4 weeks of use, no side effects from the use of the drug were registered, which indicates good tolerability.

Effectiveness of fixed combination of olopatadine hydrochloride and mometasone furoate in adults and children with allergic rhinitis in real-life clinical practice settings: results of «RYAL» prospective observational study

Effectiveness of fixed combination of olopatadine hydrochloride and mometasone furoate in adults and children with allergic rhinitis in real-life clinical practice settings: results of «RYAL» prospective observational study

Efficacy, safety, and serum cytokine modulation by olopatadine hydrochloride and desloratadine citrate disodium combination therapy in urticaria.

To assess the efficacy, safety, and impact on serum cytokines of olopatadine hydrochloride (OLP) combined with desloratadine citrate disodium (DES) in treating urticaria. We retrospectively analyzed 114 urticaria patients treated at the Affiliated Hospital of Xinyang Vocational and Technical College from March 2020 to March 2023. The control group (55 patients) received DES, while the research group (59 patients) received OLP+DES combination therapy. We compared efficacy, safety (including epigastric pain, dry mouth, lethargy, dizziness, and fatigue), changes in serum cytokines (interleukin [IL]-2, IL-4, and interferon [IFN]-γ), symptom resolution (wheal number, wheal size, and itching degree), and 3-month recurrence rates. A univariate analysis was also conducted to identify factors influencing urticaria recurrence. The research group exhibited a significantly higher overall efficacy rate, lower incidence of adverse events, and reduced recurrence rates at 3 months (all P<0.05) compared to the control group. Post-treatment, the research group showed significant increases in IL-2 and IFN-γ levels and reductions in IL-4 levels, wheal number, wheal size, and itching degree (all P<0.05). Factors such as history of drinking/smoking, IL-2 levels, and treatment method were associated with urticaria recurrence (all P<0.05). The combination of OLP and DES is an effective and safe treatment option for urticaria, significantly improving serum cytokine profiles, alleviating symptoms, and reducing recurrence risk.

Efficacy of the topical antihistamine olopatadine in dogs with experimentally induced allergic conjunctivitis

AbstractObjectiveThe objective of the study was to evaluate the efficacy of a once a day, over the counter antihistamine eye drop, 0.7% olopatadine hydrochloride, in treating or preventing experimentally induced allergic conjunctivitis in dogs.Animals studiedTwelve systemically healthy pet dogs with no known history of allergies or atopic dermatitis, and in the past 12 months had no known ocular abnormalities.ProceduresDogs were randomly assigned to two groups: “Treatment” which received topical 0.7% olopatadine hydrochloride and “Control” which received artificial tears. Dogs received the antihistamine eye drops before (Phase 1) or after (Phase 2) receiving a compounded ophthalmic histamine solution to induce clinical signs of allergic conjunctivitis. Conjunctival hyperemia, chemosis, follicles, ocular discharge, and ocular pruritus were graded, and photographs were used to document changes. Schirmer tear test values, fluorescein staining, and intraocular pressures were monitored throughout.ResultsIn both Phase 1 and Phase 2, conjunctival scores increased 10 min after histamine administration (p &lt; .05). There was no difference between maximum overall conjunctival scores between treatment and control groups in either phase or when comparing treatment groups of Phase 1 to Phase 2 (p &gt; .05). However, treatment groups in Phase 2 did have a higher maximum conjunctival chemosis score and spent more time at their maximum chemosis score when compared to Phase 1 (p &lt; .05).ConclusionOlopatadine may be beneficial as prophylaxis to reduce the degree and duration of clinical signs of allergic conjunctivitis.

Intranasal combo: fixed-dose combination of mometasone furoate and olopatadine hydrochloride in therapeutic strategies for rhinosinusitis.

A novel strategy for the treatment of allergic rhinitis results from the innovative combination of antihistamine and intranasal corticosteroid drugs. By combining two preparations with different mechanism of action, this novel approach facilitates quick and effective controls of all upper respiratory tract allergy symptoms. The article presents the results of a study of olopatadine hydrochloride and mometasone furoate fixed-dose combination (GSP301) administered intranasally from a spray formulation, with an attempt at positioning the treatment within the ARIA and EPOS guidelines.

Electro‐elucidation and quantification of olopatadine hydrochloride in bulk form and eye drops using modification free glassy carbon electrode with its development by different electrolytes and surfactants

AbstractThe electro‐oxidation pathway of olopatadine hydrochloride which is used in eye drops as antihistaminic agent was proposed and discussed in detail as the first time using different voltammetry methods at the modification free glassy carbon electrode surface. The oxidation process of olopatadine hydrochloride based on the presence of electro‐active tertiary amine group was irreversible. The dissociation constants were attained by the dependence of peak current and potential on the pH values. Some kinetic parameters were also estimated. Depending on the oxidation of olopatadine hydrochloride in citrate buffer (pH 5.5; 0.1 M) and sodium dodecyl sulfate (3×10−5 M) as supporting electrolyte and a modifier, respectively, sensitive, simple, accurate and inexpensive a novel square wave voltammetry method was achieved. The method was validated for linearity, precision, accuracy, ruggedness, specificity and stability. Limit of detection of 9×10−7 M in bulk form was attained. The characterized method was successfully used for routine analysis of olopatadine hydrochloride in pharmaceutical eye drops (Olohistine® and olopalite). No electroactive interferences from the inactive ingredients present in eye drops were noticed. So the proposed method does not necessitate any extraction step preceding the drug analysis. Also, the obtained data of the calibration curve and standard addition methods were compared statistically with a reported spectrophotometrically method showing no differences between them with respect to accuracy and precision, what proved the reproducibility, suitability and reliability of the described voltammetric method for assay of olopatadine hydrochloride in its formulation.

UV spectrophotometric methods for simultaneous determination of ketorolac tromethamine and olopatadine hydrochloride: Application of multiple standard addition for assay of ophthalmic solution

Ophthalmic preparations that contain ketorolac tromethamine (KET) and olopatadine HCl (OLO) are used to relieve seasonal allergies and allergic conjunctivitis. Simultaneous quantification of KET and OLO was held by validated and simple spectrophotometric methods. KET was determined directly from the fundamental UV absorption spectra (at 323 nm), while OLO was determined after performing either dual wavelength or ratio derivative methods. The first method was based on measuring the absorbance difference (ΔA) between 243 and 291 nm, while the second depended on generating first derivative ratio spectra using 3.0 µg/mL KET as a divisor and measuring OLO responses at 234 nm (minima). Multiple standard addition method was applied to enable the determination of OLO which is considered as the weakly absorbing species as well as the minor component in a challenging dosage form ratio (4:1). The linearity ranges of the developed methods were 3–12 μg/mL and 4–40 μg/mL for KET and OLO, respectively. Simultaneous determination of both drugs was successfully implemented to lab prepared eye drops that contain KET, OLO and benzalkonium chloride as an inactive ingredient. Greenness assessment indicates minimal impact on environment. The developed methods determined the cited drugs with % recovery ± SD of 99.63 ± 0.01 for KET, 100.90 ± 0.02 and 100.31 ± 0.01 for OLO using dual wavelength and first derivative ratio methods, respectively. Using F-test and t-test at confidence level %95 to compare between the results of the presented methods and a reported method show no significant difference which allows precise, accurate, rapid, and simple quantification of quality control samples that contain KET and OLO.

Protective effect of olopatadine hydrochloride against LPS-induced acute lung injury: via targeting NF-κB signaling pathway.

Morbidity and mortality rates associated with acute lung injury/acute respiratory distress syndrome (ALI/ARDS) are high (30-40%). Nuclear factor-kappa B (NF-κB) is a transcription factor, associated with transcription of numerous cytokines leading to cytokine storm, and thereby, plays a major role in ALI/ARDS and in advanced COVID-19 syndrome. Considering the role of NF-κB in ALI, cost-effective in silico approaches were utilized in the study to identify potential NF-κB inhibitor based on the docking and pharmacokinetic results. The identified compound was then pharmacologically validated in lipopolysaccharide (LPS) rodent model of acute lung injury. LPS induces ALI by altering alveolar membrane permeability, recruiting activated neutrophils and macrophages to the lungs, and compromising the alveolar membrane integrity and ultimately impairs the gaseous exchange. Furthermore, LPS exposure is associated with exaggerated production of various proinflammatory cytokines in lungs. Based on in silico studies Olopatadine Hydrochloride (Olo), an FDA-approved drug was found as a potential NF-κB inhibitor which has been reported for the first time, and consideredfurther for the pharmacological validation. Intraperitoneal LPS administration resulted in ALI/ARDS by fulfilling 3 out of the 4 criteria described by ATS committee (2011) published workshop report. However, treatment with Olo attenuated LPS-induced elevation of proinflammatory markers (IL-6 and NF-κB), oxidative stress, neutrophil infiltration, edema, and damage in lungs. Histopathological studies also revealed that Olo treatment significantly ameliorated LPS-induced lung injury, thus conferring improvement in survival. Especially, the effects produced by Olo medium dose (1mg/kg) were comparable to dexamethasone standard. In nutshell, inhibition of NF-κB pathway by Olo resulted in protection and reduced mortality in LPS- induced ALI and thus has potential to be used clinically to arrest disease progression in ALI/ARDS, since the drug is already in the market. However, the findings warrant further extensive studies, and also future studies can be planned to elucidate its role in COVID-19-associated ARDS or cytokine storm.