Microparticle formulation for pulmonary drug delivery of anti infective molecule for treatment of infectious diseases
Inventors
Chimote, Geetanjali Chandrashekhar • Mahajan, Girish Badrinath • Vasudevan, Aravindan • Hariharan, Sivaramakrishnan
Assignees
Foundation For Neglected Disease Research (fndr) • National Centre For Antarctic And Ocean Research (ncaor) • Priamal Enterprises Ltd
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Publication Number
US-8697653-B2
Publication Date
2014-04-15
Expiration Date
Abstract
The present invention relates to a biodegradable, inhalable microparticle formulation comprising a compound of formula I obtained by fermentation of a microorganism of the Streptomyces species (PM0626271/MTCC5447), as described in PCT application publication WO2011027290, and a biodegradable lipid for drug delivery wherein the ratio of drug (compound of formula I) to lipid is 1:15 to 1:25. The present invention also relates to the process for preparation of the formulation and to the method of treatment of pulmonary tuberculosis, multi drug resistant tuberculosis (MDRTB), methicillin resistant Staphylococcus aureus (MRSA) pneumonias and methicillin sensitive Staphylococcus aureus (MSSA) pneumonias by administering therapeutically effective amount of the formulation to a mammal in need thereof. The present invention further relates to a method of delivering the microparticle formulation to a mammal in need thereof, wherein the formulation is administered by inhalation or intratracheal instillation for pulmonary delivery.
Core Innovation
The invention relates to a microparticle formulation for drug delivery. The formulation comprises a compound of formula I and a biodegradable lipid, wherein the ratio of the compound of formula I to lipid is 1:15 to 1:25, and the formulation is biodegradable and inhalable.
The formulation is directed to inhalable biodegradable microparticles, including compositions containing DPPC as the biodegradable lipid. The document describes microparticle size, pH, osmolality, and phase transition temperature as physicochemical characteristics of the microparticles.
The disclosed use context is pulmonary delivery, including treatment of pulmonary tuberculosis, multi-drug resistant tuberculosis, and MRSA or MSSA pneumonia. Administration is described by inhalation of a therapeutically effective amount of the microparticle formulation, and the document indicates lung retention of the compound of formula I after inhalation for 24 hours and delivery targeting of alveolar macrophages.
The document describes manufacturing routes to obtain the inhalable biodegradable microparticle formulation, including solvent evaporation and solvent-free lipid self-assembly, with processing with simulated lung fluid to obtain microparticles with specified characteristics.
Claims Coverage
The independent claim recites a biodegradable and inhalable microparticle formulation comprising a compound of formula I and a biodegradable lipid with a drug:lipid ratio of 1:15 to 1:25. The inventive features in the dependent claims refine this by specifying particle size, pH, and pulmonary treatment and retention limitations.
Biodegradable and inhalable microparticle formulation with defined drug-to-lipid ratio
A microparticle formulation comprising a compound of formula I and a biodegradable lipid for drug delivery wherein the ratio of the compound of formula I to lipid is 1:15 to 1:25, wherein said formulation is a biodegradable and inhalable formulation.
Microparticle size range between 0.5 and 10 microns
The microparticle formulation has a particle size ranging between 0.5 and 10 microns.
Formulation pH range between 6 and 7
The microparticle formulation has a pH ranging from 6 to 7.
Pulmonary treatment by inhalation of a therapeutically effective amount
A method for treating pulmonary tuberculosis, multi-drug resistant tuberculosis, and MRSA or MSSA pneumonia in a mammal by administering by inhalation a therapeutically effective amount of the microparticle formulation from claim 1.
24-hour lung retention after inhalation
The method includes administering a formulation by inhalation that retains the compound of formula I in the lungs for 24 hours.
Across the claim set, the coverage centers on a biodegradable and inhalable microparticle formulation containing a compound of formula I and a biodegradable lipid at a 1:15 to 1:25 ratio, further refined by microparticle size and pH limitations. The dependent method claims cover treating pulmonary tuberculosis, multi-drug resistant tuberculosis, and MRSA or MSSA pneumonia by inhalation and include a lung retention requirement of 24 hours for the compound of formula I.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treating pulmonary tuberculosis, multi-drug resistant tuberculosis, and MRSA or MSSA pneumonia in a mammal by administering the microparticle formulation by inhalation.
Retention of the compound of formula I in the lungs for 24 hours after inhalation.
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