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Podophyllotoxin preparation resisting condyloma acuminata relapse and HPV latent infection

A technology for podophyllotoxin and latent infection, which is applied in the field of medicine and health, can solve the problems of not being able to meet the clinical application of condyloma acuminatum, unsuitable for POD mucosal targeting preparations, difficult to treat condyloma acuminatum, etc. The effect of drug degradation and good targeting

Inactive Publication Date: 2014-07-02
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug concentration of podophyllotoxin solid lipid described in the application is only 0.05%, which is far from satisfying the clinical application of genital warts, because 0.5% podophyllotoxin is one of the first-line drugs recommended by the World Health Organization (WHO) for the treatment of genital warts one
Moreover, the preparation of SLN by simple solid lipids may form dense crystals like "brick walls", and the drug-loading space of nanoparticles is very limited, so the drug-loading capacity of podophyllotoxin solid lipids is low, and Drugs are easily squeezed out and leaked during storage
Therefore, even if the drug concentration of podophyllotoxin in the above patent literature is increased to 0.5%, it is still not suitable as a mucosal targeting preparation for POD, and it is not suitable for solving the treatment difficulties of condyloma acuminata in vagina and cervix.

Method used

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  • Podophyllotoxin preparation resisting condyloma acuminata relapse and HPV latent infection
  • Podophyllotoxin preparation resisting condyloma acuminata relapse and HPV latent infection
  • Podophyllotoxin preparation resisting condyloma acuminata relapse and HPV latent infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the preparation of podophyllotoxin preparation of the present invention

[0032] In this example, the orthogonal design will be used to optimize the formula, and the emulsification evaporation-low temperature solidification method will be used to prepare 0.5% podophyllotoxin-nano lipid carrier suspension, such as figure 1 shown.

[0033] Experimental material: podophyllotoxin (Sigma company, content 98.8%).

[0034] The specific method is as follows:

[0035] Weigh 100mg of lecithin and dissolve it in 20mL of absolute ethanol, place it in a constant temperature magnetic stirrer at a temperature of 74±1°C, stir until it is fully dissolved, and the stirring speed is 1200-1500r / min. Weigh 50 mg of podophyllotoxin, 100 mg of glyceryl monostearate and 400 μL of caprylic / capric triglyceride and dissolve in 10 mL of acetone. After complete dissolution, mix the obtained ethanol solution with the acetone solution to form an oil phase.

[0036] Weigh 200mg of Brj...

Embodiment 2

[0045] Embodiment 2: Local mucosal irritation test of podophyllotoxin preparations according to the present invention

[0046] 1. Experimental materials

[0047] 1.1 Experimental animals: 36 female SD Tibet miniature pigs, aged 6 months, with a mass of (25±3) kg, provided by the Experimental Animal Center of Southern Medical University. The experimental pigs meet the standards of clean experimental animals.

[0048] 1.2 Experimental drugs:

[0049] Podophyllotoxin-nano lipid carrier suspension: obtained by the method in Example 1.

[0050] Control drug podophyllotoxin tincture (self-made): weigh 0.05g podophyllotoxin with an electronic balance, dissolve it in 10ml absolute ethanol, and prepare 0.5% podophyllotoxin tincture.

[0051] 2. Application method:

[0052] The experimental minipigs were raised in a clean environment, and the drug was applied after the miniature pigs adapted to the new environment 2 days later. After the miniature pig is anesthetized with the anest...

Embodiment 3

[0058] Example 3: Effects of podophyllotoxin preparations of the present invention on VK2 / E6E7 cell proliferation and apoptosis

[0059] Condyloma acuminatum is a sexually transmitted disease caused by human papillomavirus (HPV) infecting the anus and external genitalia. At present, the most ideal way to treat HPV infection is to directly target the virus or the cells infected by the virus and remove the virus from the cells and tissues. Clean it up completely. However, due to the lack of effective antiviral means and the difficulty of completely eradicating virus-infected cells, traditional treatment methods have a high recurrence rate. Local HPV latent infection is considered to be the main cause of recurrence of genital warts.

[0060] Since there is no mature and recognized animal model of HPV infection at home and abroad to conduct pharmacodynamic studies, the present invention uses HPV-infected human immortalized vaginal epithelial cells (VK2 / E6E7 cells) for experimenta...

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Abstract

The invention relates to a podophyllotoxin preparation resisting condyloma acuminata relapse and HPV latent infection, which is mainly used for treating condyloma acuminate of a cervix uteri, a vagina, a urethra, an anal tube mucosa and skin, HPV latent infection and the like. The podophyllotoxin preparation disclosed by the invention takes a nanostructured lipid carrier as a drug carrier material; the packaged pharmaceutical active component is podophyllotoxin; the mass-to-volume ratio of podophyllotoxin to the nanostructured lipid carrier is 0.5%. The podophyllotoxin preparation disclosed by the invention has good pro-epidermal targeting property and high physical stability and is capable of thoroughly clearing HPV infection, controlling drug release, preventing a medicine from being degraded, increasing the drug-loading capacity, etc.

Description

technical field [0001] The invention belongs to the field of medicine and hygiene, and relates to a podophyllotoxin preparation, in particular to a podophyllotoxin preparation for resisting recurrence of condyloma acuminatum and latent HPV infection, which is mainly used for treating cervical, vagina, urethra, anal canal mucosa and skin genital warts and HPV latent infection. Background technique [0002] Condyloma acuminata (CA) is one of the most common sexually transmitted diseases (STDs) caused by human papillomavirus (HPV) infection of the anus and external genitalia. It ranks second among sexually transmitted diseases. There are more than 100 genotypes of HPV, low-risk types include 6, 11, 40, 42, 43, 44, 54, 61, 70, 72, 51, ep6108 and other 12 types, which are related to external genital warts and cervical low-grade scaly There are 15 high-risk types, namely HPV16, 18, 31, 33, 35, 39, 45, 51, 52, 56, 55, 59, 68, 73 and 82 , are closely related to cervical cancer a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K9/10A61K47/14A61P31/20
Inventor 曾抗
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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