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Rifapentine-proliposomes for inhalation: in vitro and in vivo toxicity
Arpana A Patil-Gadhe1, Abhay Y Kyadarkunte1, Michael Pereira2
1Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune, India ; National Centre for Cell Sciences, University of Pune Campus, Ganeshkhind, Pune, India.
Background:
Oral therapy for pulmonary tuberculosis (TB) treatment suffers from the limitation of hepatic metabolism leading insufficient concentration of antitubercular (anti-TB) drugs in alveolar macrophage which harbors Mycobacterium tuberculosis (MTB). Targeted aerosol delivery of antituberculous drug to lung is efficient for treating local lung TB infection.
Objective:
The present study was aimed to evaluate rifapentine (RPT) loaded proliposomal dry powder for inhalation (RLDPI) for anti-TBactivity and cytotoxicity in vitro. In vivo toxicity study was also undertaken in Wistar rats to determine safe concentration of RLDPI for administration.
Materials And Methods:
Anti-TB activity of developed RLDPI was assessed using drug susceptibility testing (DST) on Mycobacteria growth indicator tube (MGIT) method. In vitro cytotoxicity was performed in A549 cell lines and IC50 values were used to compare the cytotoxicity of formulation with pure RPT. In vivo repeated dose toxicity study was undertaken using Wistar rats at three different doses for 28-days by intratracheal insufflations method.
Results:
The results of DST study revealed sensitivity of tubercle bacteria to RLDPI at concentration equivalent to 10 μg/mL of RPT. This study confirmed anti-TB potential of RPT in spray-dried RLDPI, though the spray drying method is reported to reduce activity of drugs. Cytotoxicity study in A549 cells demonstrated that RPT when encapsulated in liposomes as RLDPI was safe to cells as compared to pure RPT. In vivo toxicity study revealed that RPT in the form of RLDPI was safe at 1 and 5 mg/kg dose. However, mortality was seen at higher dose (10 mg/kg), possibly because of liver and kidney damage.
Conclusion:
Thus, these studies demonstrated safety of RLDPI for the treatment of pulmonary TB.
Insights
Rifapentine-loaded proliposomal dry powder for inhalation (RLDPI) shows promising anti-tuberculosis activity and reduced cytotoxicity. In vivo studies indicate RLDPI is safe at specific doses for pulmonary TB treatment.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Infectious Diseases
Background:
- Oral tuberculosis (TB) treatment faces challenges due to drug metabolism, limiting efficacy in macrophages.
- Targeted aerosol delivery offers a more efficient approach for pulmonary TB infection.
Purpose of the Study:
- To evaluate the anti-TB activity and cytotoxicity of rifapentine (RPT) loaded proliposomal dry powder for inhalation (RLDPI).
- To determine the safe concentration of RLDPI through in vivo toxicity studies in Wistar rats.
Main Methods:
- Anti-TB activity assessed via drug susceptibility testing (DST) using the MGIT method.
- In vitro cytotoxicity evaluated in A549 cell lines, comparing RLDPI with pure RPT.
- In vivo toxicity determined through a 28-day repeated dose study in Wistar rats via intratracheal insufflation.
Main Results:
- RLDPI demonstrated anti-TB activity at RPT concentrations of 10 μg/mL.
- RLDPI showed reduced in vitro cytotoxicity compared to pure RPT.
- In vivo studies indicated RLDPI was safe at 1 and 5 mg/kg, with toxicity observed at 10 mg/kg.
Conclusions:
- RLDPI exhibits significant anti-TB potential and improved safety profile.
- These findings support the safety of RLDPI for pulmonary TB treatment via inhalation.
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