Review
Biochemistry & Molecular Biology
Maddalena Sguizzato, Elisabetta Esposito, Rita Cortesi
Summary: Skin disorders can be treated with topical drug applications utilizing lipid-based nanosystems, including liposomes, ethosomes, transferosomes, solid lipid nanoparticles, and more. These nanosystems offer efficient delivery of drugs, potentially reducing side effects, and have the ability to administer antioxidant molecules topically. More research is needed to understand the interaction between lipid-based nanosystems and the skin, but highlighting their possibilities could benefit the scientific community.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Nuria Garros, Paola Bustos-Salgados, Oscar Domenech, Maria Jose Rodriguez-Lagunas, Negar Beirampour, Roya Mohammadi-Meyabadi, Mireia Mallandrich, Ana C. C. Calpena, Helena Colom
Summary: Atopic dermatitis (AD) is a chronic autoimmune inflammatory skin disorder. This study aimed to develop and evaluate new topical liposomal formulations loaded with the reversible Janus-associated kinase (JAK)-inhibitor, Baricitinib (BNB), for the treatment of flare ups. Three liposomal formulations were prepared using different proportions of POPC, CHOL, and CER. Physicochemical characterization, release study, permeation and retention studies, histological analysis, and irritancy tests were performed. All liposomes showed good properties and stability. The POPC:CHOL:CER formulation had the highest flux and permeation, with retention in the skin equal to POPC:CHOL. The formulations exhibited no harmful effects and showed promising results for the aim of the study.
Article
Pharmacology & Pharmacy
Despoina Despotopoulou, Nefeli Lagopati, Stergios Pispas, Maria Gazouli, Costas Demetzos, Natassa Pippa
Summary: Transdermal drug delivery systems have advantages such as patient compliance and favorable pharmacokinetic profile, but the limited skin penetration hinders their effectiveness. Nanoparticles, with their small size and physicochemical properties, show promise as penetration enhancers. Research should consider the complex anatomy of the skin and the mechanisms of penetration to achieve practical applications for skin permeability.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Pharmacology & Pharmacy
Javiana Luengo, Marc Schneider, Anna M. Schneider, Claus-Michael Lehr, Ulrich F. Schaefer
Summary: The study showed that PLGA nanoparticles can enhance the permeation of the anti-inflammatory drug flufenamic acid (FFA) through the skin, with both drug-free and drug-loaded nanoparticles increasing drug permeation. In addition, the pH values of buffered vehicles were found to influence the permeation of FFA.
Article
Instruments & Instrumentation
Heba M. K. Ebada, Maha M. A. Nasra, Yosra S. R. Elnaggar, Ossama Y. Abdallah
Summary: The study explored the feasibility of tailoring a rhein-phospholipid complex (RH-PLC) to improve the challenging physicochemical properties and skin permeability of rhein. The RH-PLC was successfully developed at a stoichiometric ratio of 1:1, showing significantly increased solubility and permeability properties compared to RH suspension. These findings suggest that the proposed RH-PLC could be a promising approach to enhance the permeability of rhein and other drugs with poor skin permeability.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Hong-My Tran, Chun-Yin Yang, Tzu-Hui Wu, Feng-Lin Yen
Summary: Recently, there has been significant development in the global market for anti-aging skin care using botanicals. Morin, a polyphenol compound, has shown pharmacological properties such as antioxidant, anti-inflammatory, and photoprotection effects. However, its poor water solubility hinders its pharmaceutical applications. This study aimed to encapsulate morin into liposomal vesicles to improve its solubility and skin penetration and evaluate its ROS inhibition and anti-aging activity. The results demonstrated that morin exhibited strong DPPH radical scavenging activity and effectively protected keratinocytes from particulate matter-induced damage by downregulating MMP-1 expression through the suppression of p-ERK and p-p38 in the MAPK pathway. Additionally, the water solubility of liposomal morin was significantly improved compared to free morin, and deformable liposomal vesicles enhanced dermal absorption. In conclusion, liposomal morin shows potential as a promising candidate for various topical anti-aging and anti-pollution products.
Article
Medicine, Research & Experimental
Silvia Franze, Francesco Rama, Paolo Rocco, Michela Debernardi, Valeria Bincoletto, Silvia Arpicco, Francesco Cilurzo
Summary: This study demonstrates the potential of controlling drug delivery in the skin by adjusting the amount of HA on the vesicle surface. Different phosphatidylethanolamine-HA conjugates impact the deformability of liposomes and the transdermal permeation of drugs, with higher HA extent favoring drug retention in the skin.
MOLECULAR PHARMACEUTICS
(2021)
Article
Medicine, Research & Experimental
Silvia Franze, Caterina Ricci, Elena Del Favero, Francesco Rama, Antonella Casiraghi, Francesco Cilurzo
Summary: This study investigated the advantages of combining proliposomes and DiMiL as drug carriers to enhance the skin penetration of CBD. Sucrose and trehalose were found to be the best carriers for spray-dried and slurried proliposomes, respectively. Cryo-EM images showed the presence of micelles in the aqueous core of lipid vesicles in the DiMiL system, and the presence of sugars did not alter the structural organization. CBD permeation through human epidermis was significantly improved when carried by DiMiL systems, and trehalose further increased the flux.
MOLECULAR PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Antoine Bernasque, Muriel Cario, Stephanie Krisa, Sophie Lecomte, Chrystel Faure
Summary: Our previous work has found that the size, elasticity, and charge of multi-lamellar liposomes (MLLs) cannot be considered independently when predicting their fate in the skin. In this study, we developed MLLs formulations containing the corticosteroid betamethasone 17-valerate (B17) to deliver the drug to specific layers of the skin. The MLLs showed high encapsulation efficiency and protected the corticosteroid from thermal degradation. We established an equation to determine the penetration depth of MLLs in artificial skin, and confirmed its accuracy through experiments on human skin samples.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2023)
Article
Oncology
Giulia Ferrari, Lisa Y. Pang, Fabio De Moliner, Marc Vendrell, Richard J. M. Reardon, Andrew J. Higgins, Sunil Chopra, David J. Argyle
Summary: Bleomycin, a chemotherapy agent, can cause severe pulmonary toxicity when administered systemically. Bleosome, a novel formulation of bleomycin encapsulated in ultra-deformable (UD) liposomes, may be a potential topical chemotherapy for non-melanoma skin cancer. The study found that Bleosome can effectively penetrate through the skin, releasing bleomycin to deeper layers and suggesting its efficacy as a topical treatment warrants further investigation.
Article
Chemistry, Multidisciplinary
Sheng Hong, Zhangwen Peng, Meiying Wu, Yichu Nie, Yunfei Yi, Hui Cai, Xian-Zheng Zhang
Summary: Extraction of multifunctional particles from human hair provides an ingenious tactic for the design and development of sunscreens, which can effectively protect skin from UV radiation and prevent potential toxicity.
Article
Engineering, Biomedical
Deepika Malhotra, Sharadwata Pan, Lars Ruether, Gerrit Schlippe, Werner Voss, Natalie Germann
Summary: A custom-made technique was reported to synthesize process-convenient skin scaffolds by tuning the mechanical properties of hydrogels based on naturally occurring polysaccharides to match rheological properties of native human skins. Mechanical parameters were studied using oscillatory shear rheology, showing significant findings on the influence of kappa-carrageenan concentration on the elastic modulus and intercycle strain-softening behavior of the hydrogels. Diffusion experiments on caffeine permeation attributes demonstrated improved barrier features with increasing kappa-carrageenan concentration, achieving comparable penetration features with commercial 3D skin models.
JOURNAL OF THE MECHANICAL BEHAVIOR OF BIOMEDICAL MATERIALS
(2021)
Article
Pharmacology & Pharmacy
Thirapit Subongkot, Tanasait Ngawhirunpat, Praneet Opanasopit
Summary: This study aimed to develop ultradeformable liposomes with fatty acids to improve the skin penetration of rosmarinic acid, and found that ULs with oleic acid significantly increased the skin penetration of rosmarinic acid via the transfollicular pathway. Confocal laser scanning microscopy observations showed that UL vesicles attach to the skin before releasing the entrapped drug to penetrate the skin.
Article
Chemistry, Multidisciplinary
Krishnaraj Somyaji Shirur, Bharath Singh Padya, Abhijeet Pandey, Manasa Manjunath Hegde, Aparna Narayan, Bola Sadashiva Satish Rao, Varadaraj G. Bhat, Srinivas Mutalik
Summary: This study formulated liposomal chlorhexidine and evaluated its penetration ability and antimicrobial efficacy in root canal treatment. The results showed that liposomal chlorhexidine had better penetration ability and higher antimicrobial efficacy, with lower cytotoxicity.
Article
Chemistry, Applied
E. Abd, J. Gomes, C. C. Sales, S. Yousef, F. Forouz, K. C. Telaprolu, M. S. Roberts, J. E. Grice, P. S. Lopes, V. R. Leite-Silva, N. Andreo-Filho
Summary: The study aimed to evaluate the potential of liposomes containing an edge activator and loaded with caffeine to enhance caffeine permeation through the skin. The results showed that the formulation with the edge activator significantly improved the caffeine permeation capability.
INTERNATIONAL JOURNAL OF COSMETIC SCIENCE
(2021)
Article
Chemistry, Medicinal
Margherita Falavigna, Mette Klitgaard, Ragna Berthelsen, Anette Muellertz, Goril Eide Flaten
Summary: A new in vitro lipolysis-permeation model was developed to predict the in vivo absorption of fenofibrate in SNEDDSs, combining intestinal lipolysis and mucus-PVPA permeation models. The model showed potential for predicting in vivo absorption data by assessing drug permeation after in vitro lipolysis, with a good correlation between in vitro and in vivo AUCs.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Margherita Falavigna, Sunniva Brurok, Mette Klitgaard, Goril Eide Flaten
Summary: The study combined high-throughput in vitro intestinal lipolysis model with mucus-PVPA in vitro permeation model to investigate the solubilization capacity and drug permeation of SNEDDSs for fenofibrate. Results showed a significant impact of in vitro lipolysis on drug solubilization and permeation profiles. The correlation between in vitro permeation data and in vivo plasma concentration in rats was excellent, indicating the predictive ability of the developed combined in vitro model for in vivo drug absorption.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Review
Pharmacology & Pharmacy
Zahari Vinarov, Bertil Abrahamsson, Per Artursson, Hannah Batchelor, Philippe Berben, Andreas Bernkop-Schnurch, James Butler, Jens Ceulemans, Nigel Davies, Didier Dupont, Goril Eide Flaten, Nikoletta Fotaki, Brendan T. Griffin, Vincent Jannin, Janneke Keemink, Filippos Kesisoglou, Mirko Koziolek, Martin Kuentz, Alan Mackie, Antonio J. Melendez-Martinez, Mark McAllister, Anette Mullertz, Caitriona M. O'Driscoll, Neil Parrott, Jadwiga Paszkowska, Petr Pavek, Christopher J. H. Porter, Christos Reppas, Cordula Stillhart, Kiyohiko Sugano, Elena Toader, Katerina Valentova, Maria Vertzoni, Saskia N. De Wildt, Clive G. Wilson, Patrick Augustijns
Summary: The review article discusses the challenges and gaps in understanding oral drug absorption processes, focusing on specific patient populations, regional differences in the gastrointestinal tract, advanced formulations, and food-drug interactions. Controversies and gaps in current knowledge are identified to pave the way for future research in the field of oral drug absorption.
ADVANCED DRUG DELIVERY REVIEWS
(2021)
Article
Chemistry, Medicinal
Lisa Myrseth Hemmingsen, Kjersti Julin, Luqman Ahsan, Purusotam Basnet, Mona Johannessen, Natasa Skalko-Basnet
Summary: In an era of antimicrobial resistance, novel treatment options are urgently needed to improve the prevention and eradication of infectious skin biofilm-producing pathogens, while enhancing wound healing. Tailoring formulations for acute skin injuries is crucial for proper skin retention and release of antimicrobials.
Article
Pharmacology & Pharmacy
Jennifer Cauzzo, Nikhil Jayakumar, Balpreet Singh Ahluwalia, Azeem Ahmad, Natasa Skalko-Basnet
Summary: The study identifies limitations of traditional methods, introduces QPM as a promising complementary technique, and successfully locates and tracks liposomes.
Article
Chemistry, Applied
Lisa Myrseth Hemmingsen, Barbara Giordani, Ann Kristin Pettersen, Beatrice Vitali, Purusotam Basnet, Natasa Skalko-Basnet
Summary: The incorporation of chlorhexidine (CHX) liposomes into chitosan hydrogel significantly enhances its antimicrobial activity, leading to effective eradication of bacteria and biofilms, with potential therapeutic applications for skin infections.
CARBOHYDRATE POLYMERS
(2021)
Article
Pharmacology & Pharmacy
Marek Soltys, David Zuza, Tereza Boleslavska, Sarah Machac Akhlasova, Martin Balouch, Pavel Kovacik, Josef Beranek, Natasa Skalko-Basnet, Goril Eide Flaten, Frantisek Stepanek
Summary: This study systematically compared the sorption of poorly aqueous soluble active pharmaceutical ingredients to different mesoporous silica carriers, and identified potential pathways for enhancing bioavailability through the rational selection of parameters.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Pharmacology & Pharmacy
Laura Victoria Schulte-Werning, Anjanah Murugaiah, Bhupender Singh, Mona Johannessen, Rolf Einar Engstad, Natasa Skalko-Basnet, Ann Mari Holsaeter
Summary: The development of multifunctional nanofibrous wound dressings containing chloramphenicol, beta-glucan, and chitosan shows promising anti-inflammatory and antimicrobial properties for the treatment of infected and exuding wounds.
Article
Pharmacology & Pharmacy
Jostein Grip, Erik Steene, Rolf Einar Engstad, Jeff Hart, Andrea Bell, Ingrid Skjaeveland, Purusotam Basnet, Natasa Skalko-Basnet, Ann Mari Holsaeter
Summary: The study focused on developing a novel sprayable wound dressing with beta-1,3/1,6-glucan as the active ingredient. The sprayable format showed promising stability, efficacy, and cytotoxicity in vitro, and was as effective as the commercial product in promoting wound healing in healing-impaired animals. The novel sprayable beta G formulation has the potential to expand the clinical use of beta G as a wound dressing.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2021)
Article
Pharmacology & Pharmacy
Ivo Laidmae, Andres Meos, Irja Alainezhad Kjaervik, Sveinung G. Ingebrigtsen, Natasa Skalko-Basnet, Kalle Kirsimae, Tavo Romann, Urmas Joost, Vambola Kisand, Karin Kogermann
Summary: The study compared the preparation of drug-loaded liposomes using two methods and found that liposomes prepared by electrospinning were smaller and more homogeneous but contained less drug. Additionally, the electrospinning method was faster for in-situ liposome preparation.
Article
Biochemistry & Molecular Biology
Philip Rainsford, B. Ravdna Sarre, Margherita Falavigna, Bjorn Olav Brandsdal, Goril Eide Flaten, Martin Jakubec, Johan Isaksson
Summary: Water/Ion NMR Detected - Phospholipid Vesicle Permeability Assay (WIND-PVPA) is a novel method for assessing lipid barrier integrity in vitro. It quantifies the permeability of water and ions to evaluate the disruptive influence of membrane-active molecules, and compares the results with molecular dynamics simulations.
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
(2022)
Article
Pharmacology & Pharmacy
Ann Mari Holsaeter, Kristina Wizgird, Iselin Karlsen, Jeanette Frimand Hemmingsen, Martin Brandl, Natasa Skalko-Basnet
Summary: This study explores different Soy-PC based docetaxel-liposome formulations to find promising lipid compositions for drug entrapment. It is found that the inclusion of cationic lipids and PEGylation can improve drug entrapment efficiency. Further investigation is needed to determine the optimal formulation for stability and in vivo performance.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Jakob Tobias Lynnerup, Jonas Borregaard Eriksen, Annette Bauer-Brandl, Ann Mari Holsaeter, Martin Brandl
Summary: As numerous new drug candidates are poorly water soluble, enabling formulations are needed to increase their bioavailability for oral administration. This study aimed to gain insight into nanoparticle characteristics and performance using an in vitro combined dissolution/permeation setup. The results showed that nanosuspensions exhibited significantly increased dissolution rates and permeation rates compared to the raw APIs.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Article
Materials Science, Biomaterials
Lisa Myrseth Hemmingsen, Barbara Giordani, Marianne H. Paulsen, Zeljka Vanic, Goril Eide Flaten, Beatrice Vitali, Purusotam Basnet, Annette Bayer, Morten B. Strom, Natasa Skalko-Basnet
Summary: The eradication of bacteria in biofilms is a major challenge in treating chronic wounds. Antimicrobial peptides and their mimics are potential options, but their clinical use is limited. A study explored the use of a synthetic mimic of an antimicrobial peptide incorporated into liposomes to improve its anti-biofilm effect and anti-inflammatory activity. The results showed that the liposomes effectively eradicated biofilms and reduced inflammation, making them a promising therapeutic option for bacteria-infected chronic wounds.
BIOMATERIALS ADVANCES
(2023)