Background: Systemic drug delivery in schizophrenia is a major challenge, owing to the Blood-brain Barrier (BBB) and P-glycoprotein related effects. Consequently, herein an attempt is made to systemically deliver the most desirable schizophrenia drug, Quetiapine Fumarate (QF) via non-invasive intranasal route using Nanostructured Lipid Carrier (NLC) approach. Materials and Methods: The desired QF loaded NLCs were developed using central composite statistical design and the developed formulations were monitored for improving QF bioavailability and their brain targeting efficacies. Results: The optimized formulation displayed a 2-fold increase (compared to virgin QF) in ex-vivo nasal diffusion at the 6 th hr, with no sign of structural damage (upon histopathological examinations). While, QF blood-brain ratio showed 10-fold increase for NLCs administered through nasal route (in comparison to intravenous route), thereby supporting prolonged retention of QF at the site of action. Similarly, the concentration of QF (in the brain) delivered via nasal route exhibited 4-fold increment at all-time points thereby supporting a potential nose to brain transport and effective bypassing of BBB. Conclusion: The results obtained infers that non-invasive intranasal route can be used as a potential alternative to conventional treatment options towards efficient management of schizophrenia.
Objective: The present study was an attempt to systemically deliver the most desirable schizophrenia drug, ziprasidone hydrochloride (ZRS) via the intranasal route using nanostructured lipid carrier (NLC) approach. Methods:The desired ZRS loaded NLCs were developed using central composite statistical design and the developed formulation was monitored for improving ZRS bioavailability and their brain targeting efficacy.Results: Pharmacokinetic studies revealed a 10 fold increase (ZRS blood-brain ratio) for NLCs administered through nasal route (in comparison to intravenous route). Similarly, the concentration of ZRS (in the brain) delivered via nasal route exhibits 4 fold increment at all-time points.Conclusion: Therefore, the obtained results suggest a potential nose to brain transport of loaded ZRS by effective bypassing of the Blood-Brain Barrier (BBB). I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s
Objective:The aim of the present study was to increase the dissolution rate of glibenclamide (GLIB) by molecular dispersion of drug in the polymeric matrix of Pluronic F-127.Methods: GLIB-loaded solid dispersions were formulated by fusion method. The formulated solid dispersions were characterized for scanning electron microscopy (SEM), X-ray diffractometry (XRD), differential scanning calorimetry (DSC), and evaluated for percentage yield, drug content, solubility, and in vitro dissolution profile, and stability studies were conducted as per International Conference on Harmonisation guidelines Q1A in stability chamber, both at intermediate and accelerated conditions. Results: Both XRD and DSC studies suggested that crystalline GLIB was converted to amorphous form after loading into carrier. SEM studies revealed that the prepared solid dispersions were in the form of irregular particles with the absence of crystalline material. Due to this conversion of crystalline to amorphous state, formulated solid dispersions had shown improved dissolution rate profile of GLIB and stability studies suggested that formulated solid dispersions showed no significant changes in appearance and also in drug content. Conclusion:Thus, from the obtained results, it can be concluded that dissolution profile of GLIB can be improved by formulating as solid dispersion.
Objective: To develop and evaluate Nevirapine (NVP) Extended release tablets for reducing the dosing frequency using Methylcellulose USP Methocel A15-LV and Hypromellose USP Methocel K4M Premium CR used as rate retarding polymers and Magnesium stearate as lubricant. Methods: Tablets were prepared by using roller compaction technique by employing Quality by Design (QbD) and Design of Experimentation (DoE) to study the effect of various process related parameters like Bulk density, Tapped density, Compressibility index, mesh size and in-vitro release data at 20th hour. Results: Obtained results had suggested that concentration of polymer had shown a potential effect over various process parameters and in-vitro drug release studies suggested that formulated tablets had shown a sustained release up to 24h when compared with marketed formulations. Conclusion: From the obtained results it can be concluded that formulation of Nevirapine ER Tablets employing QbD lead to a single dose per day in the management of HIV/AIDS.
Objective: The main objective of the study was to formulate the oral disintegrating films loaded with atenolol by solvent-casting method and to carry out its evaluation studies.Methods: The films were prepared using the film-forming hydrophilic polymer like hydroxypropyl methylcellulose (E-5) and super disintegrant like pectin in various proportions.The formulated oral films were characterized for Fourier transform infrared (FTIR) and morphological evaluations. Various physicochemical parameters such as weight variation, folding endurance, surface pH, in vitro disintegration, and in vitro dissolution studies were carried out.Results: FTIR studies revealed that there was no drug-polymer interaction. The morphological evaluation of films showed that all the films were homogenous and transparent. The folding endurance test ensured that the films had sufficient brittleness and by weight variation test, it was inferred that all the films were within the deviation. The surface pH study showed the pH of the films was around neutral pH. The drug was well distributed in all the films. The films disintegrated within 120 s and the fastest being disintegrated in 30 s. Based on all the evaluation parameters, F6 had shown optimal performance and remarkable increase in drug release of 94.38% in 2 min.Conclusion: Thus, formulated oral disintegrating films can be termed as an alternative approach to deliver atenolol.
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