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Updated: Sep 6, 2025
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Polymeric Microparticles: Synthesis, Characterization and In Vitro Evaluation for Pulmonary Delivery of Rifampicin
Faiqa Falak Naz1, Kifayat Ullah Shah1, Zahid Rasul Niazi1
1Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, Pakistan.
Abstract:
Rifampicin, a potent broad-spectrum antibiotic, remains the backbone of anti-tubercular therapy. However, it can cause severe hepatotoxicity when given orally. To overcome the limitations of the current oral therapy, this study designed inhalable spray-dried, rifampicin-loaded microparticles using aloe vera powder as an immune modulator, with varying concentrations of alginate and L-leucine. The microparticles were assessed for their physicochemical properties, in vitro drug release and aerodynamic behavior. The spray-dried powders were 2 to 4 µm in size with a percentage yield of 45 to 65%. The particles were nearly spherical with the tendency of agglomeration as depicted from Carr’s index (37 to 65) and Hausner’s ratios (>1.50). The drug content ranged from 0.24 to 0.39 mg/mg, with an association efficiency of 39.28 to 96.15%. The dissolution data depicts that the in vitro release of rifampicin from microparticles was significantly retarded with a higher L-leucine concentration in comparison to those formulations containing a higher sodium alginate concentration due to its hydrophobic nature. The aerodynamic data depicts that 60 to 70% of the aerosol mass was emitted from an inhaler with MMAD values of 1.44 to 1.60 µm and FPF of 43.22 to 55.70%. The higher FPF values with retarded in vitro release could allow sufficient time for the phagocytosis of synthesized microparticles by alveolar macrophages, thereby leading to the eradication of M. tuberculosis from these cells.
Insights
This study developed inhalable rifampicin microparticles using aloe vera for improved tuberculosis treatment. These particles offer a promising alternative to oral therapy, potentially reducing liver toxicity and enhancing drug delivery to the lungs.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Rifampicin is crucial for tuberculosis treatment but oral administration causes hepatotoxicity.
- Current oral therapies have limitations requiring novel delivery methods.
- Aloe vera is explored as an immune modulator in drug delivery.
Purpose of the Study:
- To design and characterize inhalable spray-dried rifampicin-loaded microparticles.
- To evaluate the impact of alginate and L-leucine concentrations on microparticle properties.
- To assess the potential of these microparticles for improved anti-tubercular therapy via inhalation.
Main Methods:
- Spray-drying technique used to formulate rifampicin-loaded microparticles.
- Physicochemical characterization including size, yield, and morphology.
- In vitro drug release, aerodynamic behavior, and drug content analysis.
Main Results:
- Microparticles ranged from 2 to 4 µm with 45-65% yield.
- High drug association efficiency (39.28-96.15%) achieved.
- Retarded in vitro rifampicin release observed with higher L-leucine concentrations.
- Aerodynamic analysis showed favorable emission (60-70%) and fine particle fraction (43.22-55.70%).
Conclusions:
- Inhalable rifampicin microparticles demonstrate potential for effective tuberculosis treatment.
- Formulation parameters influence drug release kinetics and aerodynamic performance.
- The developed system may enhance drug delivery to alveolar macrophages for improved M. tuberculosis eradication.
