Our comments to A Chemistry 2015 (treatment of wrinkles)

A-Chemistry (English, French, German) is concerned with nanoemulsions for treatment of wrinkles.

D1 is concerned with the treatment of deeper wrinkles (see [001]). The document discloses the use of a conjugate of botulinum protein and a medium weight polyethylene glycol in a product called TEEN-KAR. The product is offered as an aqueous solution (see [003]). This product needs to be injected in the skin, although only once a year {see [002]). D1 is totally silent about the use of botulinum protein-PEG conjugates in the form of nanoemulsions, let alone the use of such nanoemulsions in creams that can directly be applied to and massaged into the skin to treat wrinkles. Moreover, D1 indicates that also other polymers could be used for the same purpose.

D2 describes nanoemulsions that can be used in a method of cosmetic treatment of wrinkles wherein the nanoemulsion may contain a botulinum protein (see [004]). The oil phase to be used in the nanoemulsion may be selected from a number of oils, including vegetable oils modified with polyethylene glycol.  However, in Example 1 use is made of a soy oil. Moreover, D2 is as such silent about botilinum-PEG conjagulates, as well as medium weight polyethylene glycols. The nanoemulsion may also contain a surfactant, whereby the ratio surfactant to oils is between 1:1 and 1:5 (see [008]). The latter clearly differs from [014] and Table 1 in the client’s letter. 

From the client’s letter the following passages are important for drafting the different claim categories:

• Only botulinum protein-medium weigh PEG conjugates are suitable for treating wrinkles (see [007]), meaning PEGs with an average molecular weight of 2000 to 15000 Dalton are required.
• It is essential that the conjugates used should be skin-friendly (see [008]). Hence, compositions 4 and 9 are no good (see Tables 2 and 3).
• In nanoemulsions the average droplet size is at most 1000 nm (see [009] and [010]).
• The skilled person knows that for making nanoemulsions an aqueous phase and an oil phase are needed (see [012]).
• Obtaining a nanoemulsion by our method requires that the two phases are mixed and exposed to a pressure of at least 1000 bar for a period of at least 30 seconds to at most 10 minutes (see [013]).
• The nanoemulsion is stirred into a commercially available cream (see [015]).
• Suitable pipettes can be sold together with our cream as a kit (see [015], last line).

A possible set of claims can read as follows:

1. A nanoemulsion comprising an aqueous phase, an oil phase, and a conjugate of botulinum protein and a polyethylene glycol, wherein the polyethylene glycol has an average molecular weight of 2000 to 15000 Dalton, and the nanoemulsion has an average droplet diameter of at most 1000 nm.
2. The nanoemulsion according to claim 1 having an average droplet size of less than 200 nm.
3. The nanoemulsion according to claim 1 or 2, wherein no droplets are present having a diameter of more than 500 nm.
4. The nanoemulsion according to any one of claims 1-3, wherein the polytheylene glycol has an average molecular weight of 2000 to 10000 Dalton.
5. The nanoemulsion according to any one of claims 1-4, in addition comprising a surfactant, wherein the weight ratio of surfactant to oil is 2:1 or more.
6. The nanoemulsion according to claim 5, wherein the surfactant is lecithin.
7. A method for preparing a nanoemulsion according to any one of claims 1-6, comprising the steps of:
1. preparing the conjugate of botulinum protein and the polyethylene glycol;
2. adding the conjugate of botulinum protein to the aqueous phase; and 
3. mixing the aqueous phase as obtained in step (b) and the oil phase under a pressure of at least 1000 bar for a period of time of at least 30 seconds to at most 10 minutes to obtain the nanoemulsion.
8. The method according to claim 7, wherein the pressure applied in step (c) is in the range of 1500 to 2000 bar.
9. The process according to claim 7 or 8, wherein in step (c) also a surfactant is present, whereby the weight ratio of surfactant to oil is 2.1 or more.
10. A cream comprising a nanoemulsion as defined in any one of claims 1-6.
11. Kit of parts comprising the cream according to claim 10 and a pipette.
12. Method of cosmetic treatment of wrinkles wherein the cream according to claim 10 is applied to a person’s face.

Claim 1 is believed to be both novel and inventive over both documents D1 and D2. Special reference is made to Tables 2 and 3.

From Tables 2 and 3 it becomes clear that only the conjugates with medium weight PEG provide the desired results. The other polymers do not provide the desired results. Moreover, when Table 3 is compared with Table 2 it is clear that the use of the nanoemulsion has a clearly positive effect on the wrinkle reduction (compare compositions 2 and 3 with compositions 7 and 8).

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Lex

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