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Author: search.filters.author.Chitkara, DeepakSubject: search.filters.subject.Rotigotine (RTG)

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    (Re)Formulating rotigotine: a potential molecule with unmet needs
    (Future Science Group, 2023-01) Pandey, Murali Monohar; Chitkara, Deepak
    Rotigotine (RTG), a non-ergoline D3/D2/D1 dopamine receptor agonist, is indicated for Parkinson’s disease (PD) and restless leg syndrome (RLS)[1]. It also has an affinity toward serotonin (5-HT1A, 5-HT2B, and 5-HT7) and α2B-adrenergic receptors [2]. At present, RTG is commercially available as an extended-release transdermal patch since it shows poor oral bioavailability because of its extensive first-pass metabolism [3]. Although successfully marketed, RTG potential has not been fully utilized owing to the challenges and drawbacks associated with its delivery. For instance, the absolute bioavailability from the transdermal patch is reported to be only 37%. The absolute bioavailability of transdermal patches varies depending on its site of application [3]. Moreover, RTG forms crystals in the transdermal patch upon storage and shows variations in drug release and bioavailability as well
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    Self-Assembled Lecithin-Chitosan Nanoparticles Improved Rotigotine Nose-to-Brain Delivery and Brain Targeting Efficiency
    (MDPI, 2023-03) Chitkara, Deepak; Pandey, Murali Monohar
    Rotigotine (RTG) is a non-ergoline dopamine agonist and an approved drug for treating Parkinson’s disease. However, its clinical use is limited due to various problems, viz. poor oral bioavailability (<1%), low aqueous solubility, and extensive first-pass metabolism. In this study, rotigotine-loaded lecithin-chitosan nanoparticles (RTG-LCNP) were formulated to enhance its nose-to-brain delivery. RTG-LCNP was prepared by self-assembly of chitosan and lecithin due to ionic interactions. The optimized RTG-LCNP had an average diameter of 108 nm with 14.43 ± 2.77% drug loading. RTG-LCNP exhibited spherical morphology and good storage stability. Intranasal RTG-LCNP improved the brain availability of RTG by 7.86 fold with a 3.84-fold increase in the peak brain drug concentration (Cmax(brain)) compared to intranasal drug suspensions. Further, the intranasal RTG-LCNP significantly reduced the peak plasma drug concentration (Cmax(plasma)) compared to intranasal RTG suspensions. The direct drug transport percentage (DTP (%)) of optimized RTG-LCNP was found to be 97.3%, which shows effective direct nose-to-brain drug uptake and good targeting efficiency. In conclusion, RTG-LCNP enhanced drug brain availability, showing the potential for clinical application.