Delivery Systems: Liposomes Tomorrow’s vision...Today!® Introduction
ctive Concepts has built itself upon three pillars; Liposomes are microscopic spherical, self-enclosed Ainnovative technology platforms, market leading capsules in which a phospholipid bilayer sequesters customer support, and products with a purpose. We have hydrophilic materials. The phospholipid bilayer orients diligently embarked on a quest to develop complex, active based on the the polar head region assembling towards ingredients with technologies that allow formulators the aqueous phase, while the nonpolar tail orientates to make desired, sought after claims to meet the ever towards the inside of the sphere. This system allows changing market demand for new claims. With almost for encapsulation of both lipophilic and hydrophilic two decades of experience creating active ingredients, a components. The hydrophilic exterior of the bilayer reoccurring question is often how to effectively maximize protects the incorporated components from degradation the delivery to the skin. After in-depth research on while enhancing the delivery of the actives into the skin. delivery systems, Active Concepts recommends delivery Additionally, the vesicular via liposomes for enhanced penetration. structure liposomes exhibit mimic that of the skin’s own Skin, being the human body’s largest organ, is the first natural stratum corneum. line of defense against the external environment. Active This flexible vesicular ingredients affect the skin through a multitude of structure coupled with mechanisms to either deliver or propagate the specific the amphiphilic nature desired result. Extensive research has been conducted of phospholipids creates to determine how to deliver actives through the stratum a transdermal vehicle to corneum to varying depths of the skin. One conclusion deliver the encapsulated of this research has shown the preferred mechanism for materials to the preferred delivering active ingredients into the skin is by the way of Figure 1. Cross-section of a liposome destination. liposome incorporation. structure depicting lipid bilayer. Lip∙o∙some /’lipә,sōm or līpә,sōm/ Noun/Biochemistry highly organized minute spherical structures, consisting of concentric bilayered vesicles in which an aqueous volume is entirely enclosed by a membraneous lipid bilayer1
Liposomes were first described by Dr. Alec D. Bangham in The structure and amphiphilic nature allows the liposomes 1961 at Braham Institute in Cambridge. While testing the to penetrate the epidermal barrier and travel deeper than institute’s new electron microscope, negative stain added free materials to deliver the anticipated results. to dry phospholipids provided the first real evidence that the cell membrane was a bilayer lipid structure.1 A study published in DovePress on Clinical, Cosmetic, and Liposomes were then designed as artificial cell models to Investigation Dermatology titled “Phosphatidylcholine study cell membranes and interactions. Since then, vast liposomes as carriers to improve topical ascorbic acid amounts of research have detailed liposome mechanisms treatment of skin disorders” analyzed liposomes and in drug delivery, personal care, and even in food. Dior human skin penetration Science first introduced the use of liposomes in cosmetics via Franz cells. in 1986 within the well-known range Capture.2 Marketed as containing a Liposome Complex which claimed to effectively convey active ingredients into the skin in microcapsules 300 times smaller than a normal cell was the consumer’s first glimpse at liposomes in action.3
When non-encapsulated materials are placed on the skin a range of factors determine the fate of the material. Stability, solubility, lipophilicity, and size are all obstacles the active must overcome the epidermal barrier. Liposomes, which resemble the basic structures of cellular membranes, create a more beneficial interaction with skin cells. The Science
From this study, Figure 2 illustrates the penetration Within the same original research study, fluorescein, a of empty phosphatidylcholine liposomes into human lipophilic fluorescence substance, was used to monitor whole abdomen skin preparations mounted on Franz and quantify liposomal penetration through different layers cells. The Franz cells were exposed to the empty of whole human abdomen skin. Fluorescein liposomes phosphatidylcholine liposomes and photos were taken were added to the surface of whole human skin at different at 0 hours, 48 hours, and 72 hours. Oil red staining skin times followed by a surface skin wash and visualization of histology was performed to label lipids from liposomes skin fluorescein penetration by fluorescence microscopy.4 in different skin layers.4 It is visually apparent that the It was concluded that liposomes penetrated through the epidermis to the fluorescein liposomes dermis both after 48 hours and after 72 hours compared reached the epidermis to the control. after three hours of exposure and that their content, fluorescein in the free form in receptor medium of Franz cells, started reaching the dermis progressively after 20 hours which
Figure 2. Control, 48 hour, and 72 hour photo depicting penetration of can be visualized in Figure 3. Liposome encapsulate empty phosphatidylcholine liposomes into human whole abdomen skin Figure 3.4 fluorescein penetration vs. free form preparations mounted on Franz Cells. fluorescein penetration. “The evolution of liposomes is one of the most important advancements in skin care delivery systems.” -Executive Director, Product Development at Clinique
Liposomes’ proven delivery system yields a multitude of Active Concepts produces a variety of unilamellar benefits; enhancing the penetration of actives yielding vesicles employing a proprietary composition of increased efficacy, offering time release mechanisms, phospholipids utilizing high shear techniques. These protecting and delivering otherwise unstable ingredients, specifically created vesicles have a greater Zeta Potential and opening the door to the ability to target specific cells. than typical liposomes. Zeta Potential is the measure of Liposomes can differ in size with a range in diameter the electrostatic or charge repulsion between particles. between 150 - 3500nm, and they can be found in The magnitude of the Zeta Potential is indicative of the unilamellar and multilamellar forms. While multilamellar colloidal stability, a larger Zeta Potential yields higher structures are great for specific tasks, they are not stable degrees of stability. In an effort to bring this stable as raw materials or in formulations. Unilamellar vesicles delivery system to our customers, Active Concepts offers are small, exceptionally stable molecules offering high many standard liposomes. The most popular standard stability for the incorporation into personal care products. liposomes are outlined on the following pages. Liposome Free Material
Effective Transport Unable to penetrate across a barrier across a barrier
Allows for targeted Non-specific product development product efficacy
Can increase product Decreased stability stability and efficacy in-vivo, less effective Active Concepts’ Offerings Active Concepts offers many standard liposomes. Below the most popular are listed.
Product Code & Name INCI Name Function
Utilizes antioxidant protection from essential vitamins A, C, & E drastically 60104PF AC Vitamin ACE Liposome PF Water & Phospholipids & Tocopheryl Acetate & Retinyl Palmitate & Ascorbyl preventing the oxidation process to help maintain healthy cells.
Water & Butylene Glycol & Azelaic Acid & 60173 AC Azelaic Acid Liposome Lecithin & Xanthan Gum & Atelocollagen Offers anti-inflammatory, anti bacterial, anti-acne benefits by regulating the production of keratinocytes. Great for all skin types! & Sodium Chondroitin Sulfate
60134PF AC Unloaded Liposome PF Water & Phospholipids Unloaded delivery system
60124PF AC Retinol Liposome PF Water & Phospholipids & Retinol Harnesses the well known benefits of retinol and is recommended for the delivery of age-defying and antioxidant benefits.
Caffeine increases microcirculation, delivering slimming and de-puffing 60131PF AC Caffeine Liposome PF Water & Phospholipids & Caffeine benefits while helping to reduce swelling which can cause aging effects.
Encapsulated, biotechnologically derived via E. coli Epidermal Growth Water & Phospholipids & sh- 60155SH AC EGF Liposome SH Factor. Perhaps one of the best understood signaling pathways in the Oligopeptide-1 human body, EGFR promotes collagen production, reduces fine lines, conditions, and evens skin tone.
Encapsulated biotechnologically derived Epidermal Growth Factor Water & Phospholipids & rh- 60155PF AC EGF Liposome PF produced from recombinant DNA promotes collagen production, reduces Oligopeptide-1 fine lines, conditions, and evens skin tone.
Effectively delivers antioxidants to the skin while sequestering copper to down-regulate tyrosinase activity to lighten and even skin tone while 16098 AC Cinnamon Liposome Water & Cinnamomum Cassia Bark Extract & Phospholipids allowing the skin to readily absorb potent antioxidant properties for increased functionality. Active Concepts’ Offerings Active Concepts offers many standard liposomes. Below the most popular are listed.
Product Code & Name INCI Name Function 60146PF AC Co-Enzyme Q 10 Water & Phospholipids & Ubiquinone Neutralizes harmful free radicals that are one of the major causes of aging. Liposome PF
Designed to enhance the delivery of salicylic acid to provide potent benefits 60100PF AC Salicylic Acid Water & Salicylic Acid & Phospholipids in addition to improving its solubility, allowing for the creation of products Liposome PF with a luxurious and elegant feel. Active Concepts offers many standard liposomes which are listed above. However, the liposome market is dominated by custom developed liposomes to provide targeted delivery, enhanced efficacy, and a tailored consumer experience. Considering customized, liposomal product development allows formulators to create brand differentiating products and ensure optimal active delivery... a true Active Concept. Contact your Active Concepts regional sales representative to discuss your liposome custom development needs. Parameter Guidelines Storage Store in cool, dry place at room temperature. Do not expose to excess heat or cold. Formulation Temperature 45-50°C Interactions Ideal in aqueous or O/W systems Surfactant system, add after system is structured. References: 1- Deamer, David. From “Banghasomes” to liposomes: A memoir of Alec Bangham, 1921-2010. The FASEB Journal. vol. 24 no. 5 1308-1310. May 2010. 2- “Dior Science.” Dior. N.p., n.d. Web. 22 Aug. 2016. 3- “Dior Captures Essence for a Youthful Look.” New Straits Times [Malaysia] 15 Jan. 1998: 1-41. Print. 4- Milara, Javier, Gabriel Serrano, Patricia Almudever, Juan-Manuel Serrano, Ana Torrens, Inmaculada Expósito, and Julio Cor ijo. “Phosphatidylcholine Liposomes as Carriers to Improve Topical Ascorbic Acid Treatment of Skin Disorders.” CCID Clinical, Cosmetic and Investigational Dermatology (2015): 591. Dove Press. Web. 2 Aug. 2016 5- Gaspar U. M. M. Bakowsky, and C. Ehrhardt Inhaled Liposomes Current Strategies and Future Challenges vol no 3 p. 2008;4:1-13.
Active Concepts, LLC Active Concepts S.r.l. Active Concepts LLC, Asia Lincolnton, NC. USA Milano ITALY Kaohsiung, Taiwan www. activeconceptsllc.com www.activeconcepts.it www.activeconceptsllc.com Office: +1 (704) 276 7100 Tel +39 02 90360719 Tel + 886 73599900 [email protected] [email protected] [email protected] Tomorrow’s vision...Today!®