Sol-gel Technologies Ltd.

Peptor Limited

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.

Other

Develogen Israel Ltd.

Alon Seri-Levy

Shlomo Magdassi

Noa Lapidot

Chaim Gilon

David Avnir

Orit Gans

Claudio Rottman

Doron Eren

Irina Zeltser

Dan Muller

Gal Bitan

Vered Hornik

Gary Gellerman

Yoram Sorek

Claudi Rottman

Gal Gitan

Ofer Toledano

Orit Ben Zazon

A therapeutic, cosmetic or cosmeceutic composition for topical application, capable of stabilizing an active ingredient and delivering the active ingredient, comprising a plurality of microcapsules having a core-shell structure. The microcapsules have a diameter of approximately 0.1 to 100 micron. The core of each microcapsule includes at least one active ingredient, and is encapsulated within a microcapsular shell. The shell is comprised of at least one inorganic polymer obtained by a sol-gel process, and the shell protects the active ingredient before topical application and is designed to release the active ingredient from the microcapsules following application. The composition is useful in encapsulating active ingredients, such as benzoyl peroxide, that are unstable in other formulation, or are irritating to the skin.

Composition exhibiting enhanced formulation stability and delivery of topical active ingredients

A therapeutic, cosmetic or cosmeceutic composition for topical application, capable of stabilizing an active ingredient and delivering the active ingredient, comprising a plurality of microcapsules having a core-shell structure. The microcapsules have a diameter of approximately 0.1 to 100 micron. The core of each microcapsule includes at least one active ingredient and is encapsulated within a microcapsular shell. The shell is comprised of at least one inorganic polymer obtained by a sol-gel process, and the shell protects the active ingredient before topical application and is designed to release the active ingredient from the microcapsules following application. The composition is useful in encapsulating active ingredients, such as benzoyl peroxide, that are unstable in other formulation, or are irritating to the skin.

Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N(&#x3c9;-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N(&#x3c9;-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

Conformationally constrained backbone cyclized peptide analogs

The present invention generally relates to safe and stable sunscreen compositions comprising of at least one sunscreen active ingredient in the form of an inert sol-gel microcapsules encapsulating ultraviolet absorbing compounds in any acceptable cosmetic vehicle. The composition according to the present invention can comprise several ultraviolet absorbers that may be encapsulated in the same sol-gel microcapsule or in different capsules. The hydophobicity/hydrophilicity character of the sol-gel microcapsules can be controlled by selecting suitable sol-gel precursors and suitable reaction conditions and can be chosen to be compatible with the cosmetic vehicle to be used in the sunscreen composition, thus, the present invention facilitates an easy incorporation of the composite sol-gel encapsulated sunscreen in all types of cosmetic vehicles including oil free compositions, with no necessary steps of heating or high shear forces. The sunscreen compositions of the present invention can comprise any acceptable UVA and/or UVB absorbing compounds at any desired ratio to obtain a desired accumulative ultraviolet screening spectrum.

Sunscreen composition containing sol-gel microcapsules

The present invention relates to a method for obtaining improved photostability of a sunscreen composition that contains at least two sunscreen active ingredients, which are photo-unstable when formulated together, by microencapsulating at least one of said active ingredients in an encapsulating material suitable for holding the encapsulated active ingredient material, thus reducing or preventing its leaching out of the capsules; and adding other acceptable components and additives needed for the preparation of said composition. The sunscreen active ingredients can be selected from UVA and UVB absorbers, preferably a combination thereof. In a preferred embodiment of the present invention said active ingredients are encapsulated in separate sol-gel microcapsules.

Method for obtaining photostable sunscreen compositions

Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N (&ohgr;-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N (&ohgr;-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

The present invention relates to a novel process for preparing sol-gel microcapsules loaded with up to 95% (w/w) functional molecules or substances and to the products obtained by said process. Said process is conducted in two steps: (a) creating an oil-in-water emulsion by emulsification of a water insoluble solution comprising the sol-gel precursors and the molecules to be loaded, in an aqueous solution under appropriate shear forces; (b) mixing and stirring said emulsion with an aqueous solution at a suitably selected pH to obtain loaded sol-gel microcapsules in suspension. The microcapsules so obtained can further be subjected to cycles of isolation and rinsing. Incorporation of the final product, either in the form of a suspension or a powder, in cosmetic formulations affords a transparent cream when applying to skin and has a smooth and pleasant contact.

Method for the preparation of oxide microcapsules loaded with functional molecules and the products obtained thereof

Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N,(&ohgr;-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N,(&ohgr;-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

The present invention generally relates to safe and stable sunscreen compositions comprising of at least one sunscreen active ingredient in the form of an inert sol-gel microcapsules encapsulating ultraviolet absorbing compounds in any acceptable cosmetic vehicle. The composition according to the present invention can comprise several ultraviolet absorbers that may be encapsulated in the same sol-gel microcapsule or in different capsules. The encapsulation of the ultraviolet absorbers reduces or even prevents the contact between the sunscreen compounds and the human tissue, thus reducing various adverse effects that are associated with the use of sunscreens, such as photoallergy and phototoxicity, and makes the composition safer for use. The encapsulation also reduces or even prevents cross reactivity between the sunscreen compounds and the packaging material and between the sunscreen compounds and any other component present in the composition, thus enhance the compositions stability. The hydophobicity/hydrophilicity character of the sol-gel microcapsules can be controlled by selecting suitable sol-gel precursors and suitable reaction conditions and can be chosen to be compatible with the cosmetic vehicle to be used in the sunscreen composition, thus, the present invention facilitates an easy incorporation of the composite sol-gel encapsulated sunscreen in all types of cosmetic vehicles including oil free compositions, with no necessary steps of heating or high shear forces. The sunscreen compositions of the present invention can comprise any acceptable UVA and/or UVB absorbing compounds at any desired ratio to obtain a desired accumulative ultraviolet screening spectrum.

Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N.sup..alpha. (.omega.-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N.sup..alpha. (.omega.-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

Novel peptide analogs are disclosed. The novel peptides are conformationally constrained backbone cyclized somatostatin analogs. Methods for synthesizing the somatostatin analogs and for producing libraries of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs, and methods of using such compositions in the treatment of endocrine disorders, neoplasms and metabolic disorders are also disclosed.

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Jerusalem, Israel

Alon Seri-Levy