China
Africa
Explore chapters and articles related to this topic
Innovations and Future Prospects of Dermal Delivery Systems
Published in Tapash K. Ghosh, Dermal Drug Delivery, 2020
Rashmi Upasani, Anushree Herwadkar, Neha Singh, Ajay K. Banga
Transfersomes®, also termed as deformable liposomes, are elastic vesicles that consist of phospholipids and an edge activator. Typically these edge activators are single chain surfactant molecules (e.g., sodium cholate, sodium deoxycholate, Span’s and Tween’s) that destabilize and deform the lipid bilayers of the stratum corneum. Studies have reported that deformable vesicles are able to penetrate intact skin in vivo and able to deliver therapeutic amounts of a number of actives including macromolecules. Some examples include lidocaine, cyclosporine A, insulin, diclofenac, triamcinolone acetonide, levonorgesterel, ethinylestradiol and zidovudine (Elsayed et al. 2007). The ability of transfersomes to squeeze between cells in the stratum corneum under the influence of an in vivo transcutaneous hydration gradient is one of the proposed mechanisms for their ability to facilitate transdermal delivery. Figure 14.3 shows pictomicrographs from a study by Chaudhary et al. demonstrating increased permeation of the transfersomes formulations in skin layers in comparison to control vehicle formulations (Chaudhary et al. 2013). Products based on this technology are under development by a biopharmaceutical company IDEA AG. Their transfersome-based gel product for ketoprofen is currently in phase III trials in Europe for treatment of peripheral pain.
Treatment of skin with antioxidants
Published in Roger L. McMullen, Antioxidants and the Skin, 2018
The second classification of carrier is vesicular systems: liposomes, phytosomes, transfersomes, ethosomes, and niosomes. Liposomes are the most popular vesicular system used in personal care applications and are composed of concentric layers of phospholipid bilayers spherically shaped with a hollow center for the active ingredient. Phytosomes are vesicles of phospholipids that have high affinity for phytocompounds, such as polyphenols. Transfersomes are lipid vesicles that consist of fatty acids and a small amount of ethanol. They are more elastic than liposomes, which improves their deposition characteristics. Ethosomes are lipid vesicles that contain even greater amounts of ethanol, yielding a more flexible vesicle. Niosomes are lamellar vesicles based on nonionic surfactants. Due to the nature of the surfactants in niosomes, crossing the stratum corneum is more facile than in the case with other vesicles.
Nanocarriers Systems and Their Application for the Delivery of Different Phytoconstituents
Published in Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan, Novel Drug Delivery Systems for Phytoconstituents, 2020
Ebru Altuntaş, Gülgün Yener, Burcu Özkan
Transfersomes are made of an infrastructure including hydrophilic and hydrophobic parts together and consequently can incorporate high soluble drug molecules. Due to their elasticity, transfersomes can soften and cross through narrow skin channels (5 – 10 folds less than their own diameter) without significant loss (Jain, 2008, Verma et al., 2010a). A better penetration of intact vesicles can be obtained with this high deformability (Rajan et al., 2011). These are more elastic than the classic liposomes; therefore, they are used as a new carrier for effective drug delivery via transdermal route (Jain et al., 2006, Verma et al. 2010a). The easily deformable properties of transfersomes enable them to squeeze out easily from the stratum corneum, and the penetration mechanism is the formation of an osmotic gradient due to the water evaporation through the application of transfersomes on the surface of the skin (Verma et al., 2010a). Transfersomes could penetrate the stratum corneum by either the transcellular route or intracellular route (Jain, 2008, Langer, 2004, Verma et al., 2010a). Transfersomes have been prepepared with different actives as albumin (Paul and Cevc, 1995), peptides (Cevc et al., 1995), proteins (insulin) (Cevc, 2003, Yang et al., 2002), gap junction protein (GJP) (Paul et al., 1998), DNA (Mahor et al., 2007), antigens (Bal et al., 2010), nutraceuticals (Saraf et al., 2011), analgesics (Cevc and Blume, 2001), anesthetics (Planas et al., 1992), corticosteroids (Cevc et al., 1997), and sex hormones (Essa et al., 2004) and have been demonstrated to enhance considerably the amount drug penetrated through the skin (Pandey et al., 2009). The use of transfersomes does not contain any rigorous processes, and they can be used by a method that does not require occlusion (Cevc, 1996). In addition, they provide new access for examination of skin histology with a non-invasive way (Kumar et al., 2012). Preparation of transfersomes includes pharmaceutically suitable additives, is convenient for scale up, and does not need a complicated procedure (Kumar et al., 2012). They are biodegradable and biocompatible because natural phospholipids are used to prepare them similar to liposomes. They have high entrapment efficiency, which is nearly 90% in the event of lipophilic drug. Encapsulated drugs are protected from metabolic degradation (Chien, 1991, Nandha et al., 2005). Because they function as depots, they release their contents gradually and slowly. These can be preferred for both topical and systemic drug delivery. Thus, transfersomes can prolong the release, increase the transdermal flux, and improve the site specificity of bioactive molecules (Rajan et al., 2011). Transfersomes seem to be an important carrier in the drug delivery field for the future. Besides, formulations containing transfersomes have not yet gained a place in the market in large scale. These kinds of preparations have a disadvantage as being chemically unstable due to their tendency to oxidative deterioration. Another drawback that is crucial for the acceptance of transfersomes as drug carriers is the impurities that can be found in natural phospholipids (Kumar et al., 2012, Walve et al., 2011).
A transfersomes hydrogel patch for cutaneous delivery of propranolol hydrochloride: formulation, in vitro, ex vivo and in vivo studies
Published in Journal of Liposome Research, 2023
Changzhao Jiang, Rui Ma, Xiumei Jiang, Renhua Fang, Jincui Ye
Efficient cutaneous delivery systems require drugs with modest molecular weights (<500 Da) and, balanced lipophilicity (Wiedersberg and Guy 2014). The oil/water distribution coefficient for PRH has been determined to be 0.20, implying good hydrophilicity and difficulties at passively entering the blood stream in large quantities via percutaneous absorption. Encapsulation of drugs in transfersomes is a potential solution (Alshraim et al.2019). Transfersomes have a vesicular structure that is made of phospholipids and surfactants, and when applied to skin surfaces, they penetrate the intercellular area of the stratum corneum via a hydration gradient (Zhang et al.2014). This carries the drug into the skin and causes it to accumulate in subcutaneous tissues, significantly improving local drug concentrations and enhancing its curative effects (Li et al.2013). The ability of transfersomes as carriers for low and high molecular weight drugs, including analgesics, anaesthetics, corticosteroids, sex hormones, anticancer drugs, and insulin has been evaluated (Venkatesh et al.2014).
The effect of surfactant type on characteristics, skin penetration and anti-aging effectiveness of transfersomes containing amniotic mesenchymal stem cells metabolite products in UV-aging induced mice
Published in Drug Delivery, 2022
Andang Miatmoko, Nurul Ailda Marufah, Qothrin Nada, Noorma Rosita, Tristiana Erawati, Joni Susanto, Kusuma Eko Purwantari, Arif Nurkanto, Purwati , Widji Soeratri
Transfersomes represent an artificial vesicular system possessing ultra-deformable properties and an aqueous core surrounded by a double layer of phospholipids (Cevc 2004; Kamran et al. 2016). Their ability to deform enables them to pass through narrow skin pores and serve as carriers of drugs either high or low in molecular weight. They penetrate the epidermis by modifying intercellular lamellar lipids present in the stratum corneum (Cevc and Blume 1992; Imam et al. 2017). A study conducted by Surini et al. (2018) developed a transfersomal anti-aging product containing Centella asiatica extract, a transfersomal gel with twice the penetrative ability than that of the control gel, as the active cosmetic ingredient. In addition, transfersomes have also been employed as a delivery system for proteins and peptides that penetrate the skin with difficulty due to large biogenic molecules and degradation in the gastrointestinal tract when administered orally (Pawar et al., 2016)
Ratite oils for local transdermal therapy of 4-OH tamoxifen: development, characterization, and ex vivo evaluation
Published in Journal of Liposome Research, 2021
Usha Sundralingam, Saravanan Muniyandy, Ammu K. Radhakrishnan, Uma D. Palanisamy
TransfersomesTM, a new class of ultra-deformable liposomes are composed mainly of phospholipids such as phosphatidylcholine (PC), and surfactants (edge activator (EA)) which are morphologically similar to liposomes, but they differ in function as they can traverse intact skin carrying therapeutic amounts of drugs into the systemic circulation (Cevc and Blume 1992). These highly deformable vesicles are able to permeate through the pores of the stratum corneum (SC), which are one tenth of their own diameter when applied under non-occlusive conditions (Gupta et al.2012). Transfersomes are more deformable than the liposomes. The high hydrophilicity of transfersomes allows its membrane to swell more as opposed to the conventional liposomes, which helps transfersomes to avoid aggregation and fusion, which are common occurrence with liposomes exposed to osmotic stress (Jain et al.2003). Transfersomes have been used as carriers for several therapeutic agents, including proteins, insulin, DNA, nutraceuticals, and anaesthetic; where in all cases transfersomes were shown to significantly increase the amount of drug that permeated through the skin (Rai et al.2017). Topical application of transfersome-entrapped anticancer drugs to treat various kinds of cancer has also been described (El Maghraby et al.2001, Alvi et al.2011, Zeb et al.2016, Abdel-Hafez et al.2018).