title: Liquid crystalline phase as a probe for crystal engineering of lactose: carrier for pulmonary drug delivery.
abstract: 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 48 h 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 ∼ 71 μm) 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.
authors.affiliation: Bharati Vidyapeeth University, Poona College of Pharmacy, Department of Pharmaceutics, Erandwane, Pune 411038, India. Electronic address: sharvilpatil25@gmail.com.
authors.forename: Sharvil S
authors.initials: SS
authors.lastname: Patil
authors.affiliation: Bharati Vidyapeeth University, Poona College of Pharmacy, Department of Pharmaceutics, Erandwane, Pune 411038, India.
authors.forename: Kakasaheb R
authors.initials: KR
authors.lastname: Mahadik
authors.affiliation: Centre for Pharmaceutical Engineering Science, University of Bradford, Bradford BD7 1DP, UK.
authors.forename: Anant R
authors.initials: AR
authors.lastname: Paradkar
mesh_terms: D000280:Administration, Inhalation; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D004337:Drug Carriers / Q000737:chemistry*; D005989:Glycerides / Q000737:chemistry; D007785:Lactose / Q000737:chemistry*; D050866:Liquid Crystals / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D033362:Powder Diffraction; D053838:Scattering, Small Angle; D017550:Spectroscopy, Fourier Transform Infrared; D013818:Thermogravimetry; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D005989:Glycerides; C005953:monoolein; D007785:Lactose
keywords: Cascade impactor; Cubic phase; Glyceryl monooleate; Lactose monohydrate; Salbutamol sulfate