Development of Proniosomal Dry Powder Inhaler Formulations Using Different Methods


Gelmez Yıldız B., Akbal Dağıstan Ö., Yıldız Peköz A., Yüksel N.

ISOPS 14th International Symposium on Pharmaceutical Sciences, Ankara, Türkiye, 25 - 28 Haziran 2024, ss.292, (Özet Bildiri)

  • Yayın Türü: Bildiri / Özet Bildiri
  • Basıldığı Şehir: Ankara
  • Basıldığı Ülke: Türkiye
  • Sayfa Sayıları: ss.292
  • Ankara Üniversitesi Adresli: Evet

Özet

Introduction: Proniosomes are dry powder formulations created from non-ionic surfactants and water-soluble carrier particles. When exposed to water or biological fluids, proniosomes convert into niosomes (1). Proniosomes can potentially enhance pulmonary drug delivery by improving the flow and distribution of drugs (2). This study explores the development of proniosomal dry powder inhaler formulations for targeting the lungs, using various methods and optimizing aerodynamic particle size.

Materials and Methods In this research, proniosome formulations without active pharmaceutical ingredients (API) were prepared using the slurry and thin film-hydration methods. Inhalation-grade lactose, Lactohale LH 300, supplied by DFE Pharma, served as the water-soluble carrier. Span 60, a non-ionic surfactant from Sigma Aldrich, and cholesterol from Amresco were used to form the niosome structure. Magnesium stearate (MgSt) from Sigma Aldrich was added to the formulation to prevent aggregation. A Buchi rotavapor was employed for the slurry and thin film hydration methods, and a Teknosem lyophilizer was used for lyophilization. Ultrasonic bath, vortex, and probe-sonicator techniques were applied to reduce particle size. The resulting dry powder formulations were sieved using 200 mesh (77 µm) sieves. Particle size analysis of the proniosomes was conducted using laser diffraction with the Sympatec Helos H0728 device, calculating Dv10, Dv50, Dv90, and span values. Niosome particle size, polydispersity index (PI), and zeta potential were measured using a Malvern Zetasizer Pro.

Results: The average proniosome particle size (Dv50) for formulations produced via the slurry and thin film hydration methods was approximately 5 µm. Niosome particle sizes ranged from 1 to 3 µm, with PI values between 0.200 and 0.500 and zeta potential values below -40 mV. Results from measurements with the New Generation Impactor (NGI) device will be included.

Conclusions: Laser diffraction measurements showed that the dry powder formulations have particle sizes suitable for inhalation. Prototype blank formulations, to which APIs can be added, have been successfully prepared. The study concludes that further optimization will be more straightforward after incorporating the API.

Acknowledgements

This study was supported by Ankara University Scientific Research Projects Commission under the grant no: TDK-2024-3297.

References:

1.     Bayindir Z, Yuksel N (2015). Provesicles as Novel Drug Delivery Systems. Current Pharmaceutical Biotechnology,16(4):344–364.

2.     Gamal A, Saeed H, Sayed O M, Kharshoum R M,  Salem H F (2020). Proniosomal Microcarriers: Impact of Constituents on the Physicochemical Properties of Proniosomes as a New Approach to Enhance Inhalation Efficiency of Dry Powder Inhalers. AAPS PharmSciTech, 21:156.