The approach offers a comfortable dosing zone for AIDs patients, negating the requirement of consuming the formulation in a fed state due to enhancement in drugs' oral bioavailability.
Systemic and uncontrolled administration of erlotinib hydrochloride (ETB) is associated with severe toxicity. A novel targeted and extended release nanosponge (NS) was synthesized from glutathione (GHS) by a one-step reaction between β-cyclodextrin and pyromellitic dianhydride at room temperature for delivery of ETB in lung cancer. Characterization studies were performed using sophisticated instruments. In-vitro release study was performed in the presence of incremental concentrations of GHS which was analyzed using HPLC. Cell cytotoxicity study was evaluated on human lung cancer (A549) cell lines. In-vivo tumour inhibition and biodistribution of ETB-loaded GHS-NS (ETB-NS) were performed on BALB/c mice. NS obtained was spherical, size 212 ± 2.45 nm and high drug entrapment (92.34 ± 5.31%) (p < .001). In-vitro extended drug release (76.89 ± 0.1% release at 168 h), which was directly proportional to the concentration of GHS, demonstrated tumour targeting. There was enhanced in-vitro cytotoxicity and 97.5% inhibition in tumour growth on administering NS when compared to plain ETB (48% inhibition) indicating targeting of NS to the tumour site. Biodistribution study and in-vivo tumour growth inhibition study revealed drug release to the cancerous cell, thus preventing unnecessary drug exposure. ETB-NS exhibits extended drug release proportional to the external GSH concentration.
Background: Many researchers have prepared and evaluated nanosponges and claimed their advantages as an effective drug carrier, especially it was observed prominently in case of anti-fungal drugs. The materials employed to synthesize nanosponges were mainly crosslinking agents, different beta-cyclodextrin and other cellulose-based polymers. Many of them had used ratio proportions of cross-linking agents, d polymers to synthesize these nanosponges which ultimately produce a porous mesh-like network known as nanosponges where actually drug is encapsulated or loaded. Objective: In the present investigation, we observed the effect of various levels of crosslinking agents and beta-cyclodextrin concentrations on porosity, drug encapsulation, zeta potential and drug release by employing the quality by design approach to synthesize nanosponges rather than merely keeping both concentrations in proportions. Methods: We have slightly modified the method reported earlier i.e. melting method in which we have used rota evaporator receiver vessel for melting cross-linking agent and beta- cyclodextrin, rotated at 20 RPM at 100°C. Results: In a quality by design approach, we observed that out of four dependent variables i.e. porosity, drug loading, zeta potential and drug release, three significantly depend on the crosslinking of beta-cyclodextrin molecules which is highly appreciated by the amount of cross-linking agent present in the reaction. The pharmacokinetics of Imatinib loaded optimized nanosponges were compared with the reference product to observe the pattern of absorption and disposition. Conclusion: Nanosponges synthesized by optimization technique could be effective means of anti-cancer drug oral administration as they encapsulate the drug effectively and offer a prolonged release of drug which gradually releases the drug and avoids unnecessary exposure of the drug.
A simple, reproducible and efficient High Performance Thin Layer Chromatography method was developed for Lisinopril dihydrate in bulk drug and dosage form. A constant application rate of 0.1 ml/s with nitrogen aspirator was used, and the space between two bands was 6 mm. The slit dimension was 5 × 0.45 mm, and the scanning speed was 10 mm/s. The mobile phase consisted of n-butanol: methanol: ammonia in the ratio of 3.0: 1.0: 1.0 (v/v/v). The retention time (min) and linearity range (μl) for Lisinopril was (0.20) and (1-5) respectively. The method so developed was validated for its accuracy and precision. The LOD and LOQ were found to be 0.050237 and 0.152233 for Lisinopril respectively. The accuracy was found to be 98.88%. The developed method was found to be accurate, precise and selective for determination of Lisinopril in bulk and dosage form.
An HPLC method for Tamsulosin was developed by using a quality by design (QbD) novel concept. QbD has gained importance in recent times due to regulatory requirements in industrial application. Chromatographic separation of Tamsulosin was carried out by using C8 column, and mobile phase used was methanol and distilled water (40:60 v/v) for proper separation process. Separation by using water as a solvent is beneficial as it is cost effective process and industrially applicable. In the development of the HPLC method, factors like injection volume, conc. of methanol, the column vent temperature is critical in maintaining. Hence the Box-Behnken optimization model was applied for the main, interaction and quadratic effects of these three factors on the selected response. The effect of these parameters was studied on the tailing factor (resolution). Results were analysed during a surface diagram. Verification of the software-generated result was done by taking six replicates of the run. Finally, the method was validated according to ICH guidelines.
A simple, reproducible and efficient reverse phase high performance liquid chromatographic method was developed for Lisinopril in bulk drug and formulation. A column having 150 × 4.6 mm in isocratic mode with mobile phase containing acetonitrile: phosphate buffer (70:30; adjusted to pH 3.0) was used. The flow rate was 0.8 ml/min and effluent was monitored at 216 nm. The retention time (min) and linearity range (μg/ml) for Lisinopril was (1.510) and (10-35). The developed method was found to be accurate, precise and selective for determination of Lisinopril in bulk and formulation.
The aim of the present study was to design the mouth dissolving film of Rosuvastatin calcium (RC) by applying quality by design (QbD) approach. The mouth dissolving film was prepared using solvent casting method. The critical quality attributes (CQAs) and quality target product profiles (QTPP) of RC mouth dissolving films were defined based on previous studies. Plackett-Burman experimental design was used for initial screening of process and formulation variables. The screened variables were further optimized using 3 2 full factorial designs. The variables influencing formulation of film was HPMC E5 and PVP K30. The design space was determined using statistical tool and optimized formulations were prepared within the design space. The optimized films showed all the evaluation parameters within the QTPP. The results indicated that as long as formulation variables remain within the design space, mouth dissolving film of RC with desired characteristics and quality requirement could be formulated.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.