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Skin Absorption Booster for Timolol

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Infantile hemangioma (IH) is a common type of benign (non-cancerous) vascular tumour that typically appears within the first few weeks of an infant’s life. Characterised by a proliferation of blood vessels, IH can manifest on the skin or in internal organs.

These hemangiomas often present as raised, red or purplish areas on the skin, sometimes referred to as “strawberry marks” due to their color and texture.

Hemangiomas can be classified into two main types:

  • Topical or Superficial Hemangiomas: These are located on the skin’s surface and are commonly known as “strawberry hemangiomas.” They are easily visible and palpable, presenting as bright red, raised areas.
  • Deep or Subcutaneous Hemangiomas: These are situated deeper under the skin and may appear as bluish or skin-colored swellings. While less visible on the surface, they can be felt as lumps beneath the skin.

Timolol, a beta-blocker medication, is widely used to treat conditions such as high blood pressure (hypertension), glaucoma, and certain types of IH.

While topical timolol is effective for treating superficial hemangiomas and small lesions, it is less known for deeper subcutaneous hemangiomas – it was not found in prior recommendations for subcutaneous hemangiomas as a topical treatment.

In May 2024, Wuhan Conform Pharmaceutical Co Ltd was granted UK patents GB2600633B and GB2621775B. These patents, titled “Transdermal Permeation Enhancing Composition and Application Thereof in Timolol Preparation,” introduce a novel transdermal permeation-enhancing composition that significantly improves the skin absorption of timolol for topical use.

In other words, the patented composition has been designed to improve transdermal drug delivery, making Timolol more effective for treating conditions like infantile hemangioma.

GB2600633B:

Components: a composition consisting of timolol and a transdermal permeation enhancing composition.

The transdermal permeating enhancing composition consists of:

  • white Vaseline® (65 to 95 wt.%);
  • wax substance (5 to 35 wt.%);
  • the wax substance is either light liquid paraffin and white beeswax or white beeswax alone, and where the white beeswax is present in an amount of approximately 5 wt.%.

GB2621775B:

Components: a composition comprising timolol as an active ingredient, and a transdermal permeation enhancing composition for use in treating infantile hemangiomas.

The transdermal permeating enhancing composition consists of:

  • white Vaseline® (68 to 93 wt.%)a light liquid paraffin (5 to 30 wt.%) and white beeswax (2 to 8 wt.%).

The composition may further comprise one or more of metoprolol or propranolol.

The amount of timolol in both of the patented compositions may be between 0.1 to 3 wt.%.

The patents also claim an ointment comprising the compositions.

These patents show that these compositions including Vaseline® may act as a base or carrier that not only helps in the formulation of an ointment, but which also enhances the ability of Timolol to penetrate through the skin’s outer layer more effectively.

It may be that the compositions form a barrier on the skin that can help retain moisture and potentially enhance the absorption of active ingredients by maintaining a hydrated environment on the skin’s surface.

UK Patent Law and Medical Treatments:

The UK Patents Act 1977 excludes methods of treatment by surgery or therapy from patentability, but substances and compositions and new uses can be patented. The new patents for timolol treatment illustrate how innovative formulations can be patented under these guidelines.

Trade mark Considerations:

The inclusion of a registered trade mark, such as Vaseline®, in patent claims can present challenges. Since Vaseline® is a trademark owned by Unilever, any modifications to the product by its owner could potentially impact the scope and interpretation of the patent claims. This underscores the importance of careful consideration in patent drafting and the need for clarity regarding the use of branded components in patent applications.

Patent History:

The patent application process began with a priority filing in China (CN201910846541) on 4.9.2019, followed by an international PCT application on 18.9.2020.

After the international application entered into the national phase, the first (parent) UK application (GB2201671.1) was lodged on 9.2.2022 and granted as GB2600633B on 3.4.2024. The second (divisional) application (GB2318187.8) was lodged on 29.11.2023 and granted as GB2621775B on 15.5.2024.

For more information on patent timelines and how quickly a patent can be granted, click here; and for divisional applications and recent changes under UK law, click here.

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