Dry-Powder Inhaler Formulation of Rifampicin: An Improved Targeted Delivery System for Alveolar Tuberculosis

Journal of Aerosol Medicine and Pulmonary Drug Delivery
Tejal RawalShital Butani

Abstract

The delivery of antitubercular drugs through direct lung targeting can lead to reduction in the dose as well as side effects of the drug. In the present investigation, carrier (lactose)-based dry-powder inhaler of rifampicin was prepared to achieve direct targeting of the drug into the lungs. The dry powder inhaler formulation was prepared by simply mixing micronized rifampicin with coarse and fine lactose preblend. Preliminary blends of the drug were prepared with various lactose grades (Inhalac®, Respitose,® and Lactohale®). Rotahaler® and Revolizer® were evaluated for the performance. The 32 factorial design was used to optimize the amount of drug (X1) and amount of fine lactose (X2). In vitro lung deposition was carried out using Andersen Cascade Impactor. The % cell viability studies of the formulation were carried out using murine macrophage J774 cell lines. The in vivo toxicity was determined using histopathology. Further in vivo pulmonary pharmacokinetics of the developed dry-powder inhaler (DPI) formulation was carried out in comparison to the marketed formulation in the rat lungs. Based on preliminary trials, Inhalac 230 and Inhalac 400 were selected as coarse and fine lactose grades, respectively. Rotahaler® exhibite...Continue Reading

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Methods Mentioned

BETA
infrared spectroscopy
Scanning Electron Microscopy

Software Mentioned

Copley Inhaler Testing Data Analysis Software ( CITDAS
Design expert

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