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1.
AAPS PharmSciTech ; 23(4): 99, 2022 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-35338414

RESUMO

Isoniazid (INH) is a first-line chemotherapeutic drug employed in the management of tuberculosis. However, its extensive first-pass metabolism, short-life life, and low oral bioavailability confined its medical application. Therefore, the calcium ion-alginate-piperine microspheres (INH-CaSP Ms) was prepared to enhance encapsulation efficiency, controlled delivery, and oral bioavailability of INH. The INH-CaSP Ms was developed using a modified emulsification method and optimized via Box-Behnken design (BBD). Optimized INH-CaSP Ms were characterized for encapsulation efficiency, differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), bio-adhesion, in vitro dissolution, ex vivo permeation, and oral bioavailability studies. Characterization studies confirmed the formation of microspheres. The INH-CaSP Ms showed spherical microspheres with enhanced encapsulation efficiency (~ 93.03 ± 1.54% w/w). The optimized INH-CaSP Ms exhibited higher bio-adhesion around (~ 81.41 ± 1.31%). The INH-CaSP Ms enhanced the dissolution rate of INH (~ 57%) compared to pure INH (~ 57%) and INH-SA Ms (~ 81%) in simulated gastric fluid (SGF, pH 1.2) and simulated intestinal fluid (SIF, pH 7.4). The same formulations improved the permeation rate of INH (~ 90%) compared to pure INH (~ 55%) and INH-SA Ms (~ 80%). The oral bioavailability results indicated that INH-CaSP Ms appreciably improved the oral bioavailability of INH via increasing the Cmax, Tmax, t1/2, and AUC parameters compared to pure INH. The study demonstrates that the development of INH-CaSP Ms via cross-linked coordinate bond interaction between divalent cation calcium ion-alginate complex and anion piperine bio-enhancer is an effective approach for enhancing the encapsulation efficiency, bio-adhesion, controlled release, and oral bioavailability of INH.


Assuntos
Cálcio , Isoniazida , Alginatos/química , Alcaloides , Benzodioxóis , Disponibilidade Biológica , Microesferas , Piperidinas , Alcamidas Poli-Insaturadas , Espectroscopia de Infravermelho com Transformada de Fourier
2.
J Ayurveda Integr Med ; 3(3): 164-7, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-23125515
3.
J Ayurveda Integr Med ; 2(4): 211-6, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22253513

RESUMO

Dr. Ashok D.B. Vaidya, the stalwart in the fields of Experimental Pharmacology, Clinical Pharmacology, and Reverse Pharmacology turns 75 on Nov, 27, 2011. A former Clinical Research Head of CIBA Geigy Research Centre, his name has been synonymous with the concept of the Golden Triangle for resurgence of Ayurveda and its reinterpretation in modern scientific terms. At a time when most fields are populated by intellectual dwarfs and unethical operators, he stands like a giant-a scientist, a philosopher, and an ardent fighter for ethical values. In this free-wheeling interview with Ravindra R.Pandharinath, he discusses the milestones in his life, his inspirations, and dreams for the confluence of modern science, modern medicine, and Ayurveda as the new health care model for the 21st century.

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