Chloroquine gel and preparation method and application thereof
Inventors
XIE, Longxu • Li, Xiangling • Yuan, Manli • Wang, Ting • Wang, Jianyu
Assignees
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Publication Number
US-11147773-B2
Publication Date
2021-10-19
Expiration Date
Abstract
A chloroquine gel and a preparation method and application thereof. A chloroquine nanosphere includes a water-soluble nanosphere carrier, and chloroquine or a chloroquine derivative, wherein a mass ratio of the chloroquine or the chloroquine derivative to the water-soluble nanosphere carrier is no more than 1:3.
Core Innovation
The invention provides a chloroquine nanosphere in which chloroquine or a chloroquine derivative is loaded into a water-soluble nanosphere carrier. The water-soluble nanosphere carrier is water-soluble chitosan, and the chloroquine derivative is selected from hydroxychloroquine, chloroquine phosphate, or chloroquine sulfate.
The water-soluble chitosan has a deacetylation degree ranging from 80% to 95% and a viscosity-average molecular weight ranging from 3000 to 5000 g/mol. The mass ratio of the chloroquine or chloroquine derivative to the water-soluble nanosphere carrier during preparation ranges from 1:3 to 1:5, with a loading rate of 3.0% to 21.6% in the prepared chloroquine nanosphere.
The document additionally contemplates chloroquine-loaded water-soluble chitosan gel formulations for external genitalia infections and HPV-related warts. The reported characterization includes particle diameter in the range of about 100–800 nm, and the document reports reduced skin irritation compared with a chloroquine phosphate gel, improved pathology in herpes virus vaginitis and HPV condyloma acuminatum, and inhibition of multiple vaginal pathogens including HSV-2 and other bacteria and parasites.
Claims Coverage
The only independent claim is clm-00001. It contains multiple inventive features defining a chloroquine nanosphere by carrier identity, specific chitosan physicochemical ranges, and quantitative preparation and loading constraints, together with the selection of the chloroquine derivative.
Chloroquine nanosphere with water-soluble chitosan carrier
A chloroquine nanosphere comprising a water-soluble nanosphere carrier and chloroquine or a chloroquine derivative, wherein the water-soluble nanosphere carrier is water-soluble chitosan.
Specific chloroquine-to-chitosan mass ratio
The mass ratio of the chloroquine or the chloroquine derivative to the water-soluble nanosphere carrier during preparation ranges from 1:3 to 1:5.
Specific loading rate range
A loading rate of the chloroquine or the chloroquine derivative in the prepared chloroquine nanosphere ranges from 3.0% to 21.6%.
Chitosan deacetylation degree and molecular weight ranges
The water-soluble chitosan has a deacetylation degree ranging from 80% to 95% and a viscosity-average molecular weight ranging from 3000 to 5000 g/mol.
Chloroquine derivative selection
The chloroquine derivative is selected from one or more of hydroxychloroquine, chloroquine phosphate or chloroquine sulfate.
Defined emulsion/precipitation/centrifugation preparation workflow
A method for preparing the chloroquine nanospheres by forming an oil-in-water system with an aqueous phase and an oil phase matrix using a selected emulsifier, then adding a sodium hydroxide–n-propanol precipitant, followed by standing, dehydration, high-speed centrifugation, cleaning, and drying to obtain the chloroquine nanospheres.
Overall, the claims cover a chloroquine nanosphere defined by a water-soluble chitosan carrier with specified deacetylation degree and viscosity-average molecular weight, loaded with chloroquine or a specified chloroquine derivative under defined mass-ratio and loading-rate ranges. The dependent claims further narrow preparation by defining an emulsion/precipitation/centrifugation workflow.
Stated Advantages
Mucosal adhesiveness.
Local retention.
Self-degradability.
Reduced skin irritation.
Sustained release.
Improved safety.
Documented Applications
External genitalia infections, including viral vaginitis such as herpes virus vaginitis and HPV-related warts such as condyloma acuminatum.
Bacterial vaginosis and fungal-infectious vaginitis, including candida vaginitis [preliminary clinical observations].
Inhibition/management contexts for multiple vaginal pathogens, including HPV-associated conditions and infections involving HSV-2, Trichomonas vaginalis, and other listed vaginal pathogens, as reported in vitro and in vivo [as described in the document].
Preliminary clinical research in women with candida vaginitis and HPV wart patients, reporting lack of adverse reactions and higher effective rates.
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