Mon, 18 Dec 2017

Submicronic Salbutamol Respiratory Fluid: A Novel Formulation for Treating Broncho Contrictive Diseases

Virendra Pratap Singh Rathor1, Pradeep Kumar Chugh1, Anuj Bhatnagar3, Syed Ehtaishamul Haque2, Aseem Bhatnagar1, Gaurav Mittal1*

1. Dept of Nuclear Medicine, Institute of Nuclear Medicine and Allied Sciences, Defence R&D Organization, Delhi India

2. Dept of Pharmacology, Faculty of Pharmacy, Jamia Hamdard, New Delhi India

3. Rajanbabu Institute of Pulmonary Medicine and Tuberculosis, Kingsway Camp, Delhi India


ABSTRACT

Context: Inhalation of drugs like salbutamol sulphate (SBS) suffers from low pulmonary deposition due to its micronized size. Objective: (a) to develop submicronic-SBS respiratory fluid, (b) pre-clinical toxicity study, (c) in-vitro and in-vivo evaluation in terms of respiratory fraction, and (d) clinical study to assess safety and efficacy. Methods: Formulation was optimized on basis of particle size and in-vitro nebulization rate. Anderson cascade impaction (ACI) was done to validate its advantage in terms of respirable fraction. Effect on cardiopulmonary parameters (spirometry, pulse-oxymetry, echocardiography and 6-minute walk test) was evaluated and compared with control (n=12). In-vivo pulmonary deposition pattern was compared using gamma scintigraphy. Results: Formulation was optimized with average particle size of 410nm. SBS was radiolabeled with Tc-99m and 99mTc-SBS was found suitable for estimating in-vivo SBS deposition. Preclinical toxicity studies in two-animal species showed no biochemical or behavioural toxicity. In-vitro ACI data showed high respirable fraction (81.7±7.1%) in comparison to control (42.5±3.8%). In-vivo scintigraphy suggested significantly higher pulmonary deposition for test formulation in comparison to control. Better improvement in cardiopulmonary parameters was seen in test treated group. Conclusions: As demonstrated for SBS, nano-sizing may enhance regional pulmonary deposition and provide an attractive therapeutic option for bronchopulmonary disorders like COPD.

Keywords: Chronic obstructive pulmonary disease; submicronic salbutamol sulphate; nebulization; gamma scintigraphy


[PDF]  Viewed: 724  Downloaded: 71
  • Call for paper

    American Journal of PharmTech Research (AJPTR) is a peer-reviewed, bimonthly official international journal allowing access to abstracts and full-text.

    Read more...

     

  • Email & SMS Alerts

    Email/SMS alert system is one of the key features and gives update information about the submitted manuscript.

    Read more...

  • Article Statastics

    American Journal of PharmTech Research (AJPTR) provides unique facility for authors to know popularity of articles on basis of numbers of PDF download and views. It will display in tabulated format.

  • Online Submission

    American Journal of PharmTech Research (AJPTR) is one of the International open access journal devoted to various disciplines in science and technology.

    Read more...

web counter
web counter