Liquid crystalline phase as a probe for crystal engineering of lactose: Carrier for pulmonary drug delivery

• Published in: European journal of pharmaceutical sciences Vol. 68; pp. 43 - 50
• Main Authors: Patil, Sharvil S., Mahadik, Kakasaheb R., Paradkar, Anant R.
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 20-02-2015
• Subjects: Administration, Inhalation; Calorimetry, Differential Scanning; Cascade impactor; Chemistry, Pharmaceutical; Crystallization; Cubic phase; Drug Carriers - chemistry; Glycerides - chemistry; Glyceryl monooleate; Lactose - chemistry; Lactose monohydrate; Liquid Crystals - chemistry; Microscopy, Electron, Scanning; Particle Size; Powder Diffraction; Salbutamol sulfate; Scattering, Small Angle; Spectroscopy, Fourier Transform Infrared; Thermogravimetry; X-Ray Diffraction; Lactose monohydrate; Cascade impactor; Glyceryl monooleate; Cubic phase; Salbutamol sulfate
• ISSN: 0928-0987; 1879-0720
• DOI: 10.1016/j.ejps.2014.11.007

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The current work was undertaken to assess suitability of liquid crystalline phase for engineering of lactose crystals and their utility as a carrier in dry powder inhalation formulations. Saturated lactose solution was poured in molten glyceryl monooleate which subsequently transformed into gel. The gel microstructure was analyzed by PPL microscopy and SAXS. Lactose particles recovered from gels after 48h were analyzed for polymorphism using techniques such as FTIR, XRD, DSC and TGA. Particle size, morphology and aerosolisation properties of prepared lactose were analyzed using Anderson cascade impactor. In situ seeding followed by growth of lactose crystals took place in gels with cubic microstructure as revealed by PPL microscopy and SAXS. Elongated (size ∼71μm) lactose particles with smooth surface containing mixture of α and β-lactose was recovered from gel, however percentage of α-lactose was more as compared to β-lactose. The aerosolisation parameters such as RD, ED, %FPF and % recovery of lactose recovered from gel (LPL) were found to be comparable to Respitose® ML001. Thus LC phase (cubic) can be used for engineering of lactose crystals so as to obtain particles with smooth surface, high elongation ratio and further they can be used as carrier in DPI formulations.