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-11564891-B2
Publication Date
2023-01-31
Expiration Date
Abstract
A product for preventing and treating external genitalia infection and/or flat warts is provided, wherein the product comprises a chloroquine nanosphere. The chloroquine nanosphere comprises a water-soluble nanosphere carrier, and chloroquine or a chloroquine derivative. A mass ratio of the chloroquine or the chloroquine derivative to the water-soluble nanosphere carrier during preparation ranges from 1:3 to 1:5. A loading rate of the chloroquine or the chloroquine derivative in the prepared chloroquine nanosphere ranges from 3.0% to 21.6%. The water-soluble nanosphere carrier is water-soluble chitosan; a deacetylation degree of the water-soluble chitosan ranges from 80% to 95%, and a viscosity-average molecular weight thereof ranges from 3000 to 5000 g/mol. The chloroquine derivative is selected from one or more of hydroxychloroquine, chloroquine phosphate or chloroquine sulfate.
Core Innovation
The document describes a product for preventing and treating external genitalia infection and/or flat warts that comprises chloroquine nanospheres. The chloroquine nanospheres include a water-soluble nanosphere carrier and chloroquine or a chloroquine derivative, and the product uses formulation embodiments such as a chloroquine-chitosan gel and a chloroquine-chitosan gel matrix.
The water-soluble nanosphere carrier is water-soluble chitosan with a deacetylation degree ranging from 80% to 95% and a viscosity-average molecular weight ranging from 3000 to 5000 g/mol. During preparation, the mass ratio of the chloroquine or the chloroquine derivative to the water-soluble nanosphere carrier ranges from 1:3 to 1:5, and the loading rate of the chloroquine or the chloroquine derivative in the prepared chloroquine nanosphere ranges from 3.0% to 21.6%.
The chloroquine derivative is selected from one or more of hydroxychloroquine, chloroquine phosphate, or chloroquine sulfate. The document further describes a preparation workflow involving an aqueous phase and an oil phase to form an emulsion followed by precipitation using a sodium hydroxide–n-propanol precipitant, and states that the approach is intended to control release and improve performance at external genitalia infection sites, including flat warts and relevant genitalia infections.
The background problem being solved is that external genitalia infection and/or flat warts require a product that can prevent and treat those conditions while addressing limitations such as irritation and inadequate retention at mucosal sites. The document positions the chloroquine nanosphere product as a way to provide local effect and improved outcomes for external genitalia infection and/or flat warts.
Claims Coverage
The document provides one independent claim, covering the core product definition for preventing and treating external genitalia infection and/or flat warts using chloroquine nanospheres with specified carrier, ratio, loading, and derivative selection. Dependent claims refine the product by adding quantitative composition constraints and limiting the dosage form and preparation-related parameters.
Product for preventing and treating external genitalia infection and/or flat warts with chloroquine nanospheres
A product comprising chloroquine nanospheres, wherein the chloroquine nanospheres comprise a water-soluble nanosphere carrier and chloroquine or a chloroquine derivative; 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; the loading rate of the chloroquine or the chloroquine derivative in the prepared chloroquine nanosphere ranges from 3.0% to 21.6%.
Water-soluble chitosan carrier with specified deacetylation and viscosity-average molecular weight
The water-soluble nanosphere carrier is water-soluble chitosan having a deacetylation degree from 80% to 95% and a viscosity-average molecular weight 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.
Quantitative chloroquine nanosphere fraction in the product
The product of the independent claim is characterized by chloroquine nanospheres having a weight fraction ranging from 1% to 6% of the product total weight.
Gel dosage form
The product is provided as a gel dosage form.
Overall, claim coverage centers on a chloroquine-nanosphere external genitalia infection and/or flat-wart product defined by chloroquine nanospheres with a water-soluble chitosan carrier, specific mass ratio and drug loading ranges during preparation, and specified chitosan deacetylation and viscosity-average molecular weight, with derivative selection limited to hydroxychloroquine, chloroquine phosphate, and chloroquine sulfate. Dependent claims further constrain the product by specifying a nanosphere weight fraction and a gel dosage form.
Stated Advantages
Reduced irritation.
Mucosal adhesiveness and local retention.
Controlled release.
Synergistic antibacterial and antiviral effects.
Improved wound healing.
Documented Applications
Preventing and treating external genitalia infection and/or flat warts, including herpes virus vaginitis and HPV condyloma acuminatum.
In vitro inhibition of vaginal pathogens and HSV-2.
Preliminary clinical research outcomes for external genitalia warts, including that warts fall off and no reported adverse effects.
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