Epidermal Delivery of Retinyl Palmitate Loaded Transfersomes: Penetration and Biodistribution Studies

The alteration of retinoids levels in the skin can cause different disorders in the maturation of epithelial skin cells. Topical administration of these lipophilic molecules is a challenge that can be addressed by encapsulation into drug delivery systems. In this study, retinyl palmitate transferosomes formulated in cream were developed and the increases in the penetration of the active ingredients as well as the biodistribution were evaluated in vitro and in vivo. Transfersomes demonstrated a significant increase in the administration of retinyl palmitate to the epidermis by quantification of the active ingredients in the different layers of the skin, as well as by fluorescence microscopy of biopsies of non-dermatomized pig-ear skin. These results suggest that transfersomes may be an efficient vehicle for the delivery of retinoids to inner layers of the skin, such as the epidermis.

Download Full-text

Advanced Static and Dynamic Fluorescence Microscopy Techniques to Investigate Drug Delivery Systems

Pharmaceutics ◽

10.3390/pharmaceutics13060861 ◽

2021 ◽

Vol 13 (6) ◽

pp. 861

Author(s):

Jacopo Cardellini ◽

Arianna Balestri ◽

Costanza Montis ◽

Debora Berti

Keyword(s):

Drug Delivery ◽

Fluorescence Microscopy ◽

Drug Delivery Systems ◽

Laser Scanning ◽

Super Resolution ◽

Laser Scanning Confocal Microscopy ◽

Delivery Systems ◽

Scanning Confocal Microscopy ◽

Biological Phenomena

In the past decade(s), fluorescence microscopy and laser scanning confocal microscopy (LSCM) have been widely employed to investigate biological and biomimetic systems for pharmaceutical applications, to determine the localization of drugs in tissues or entire organisms or the extent of their cellular uptake (in vitro). However, the diffraction limit of light, which limits the resolution to hundreds of nanometers, has for long time restricted the extent and quality of information and insight achievable through these techniques. The advent of super-resolution microscopic techniques, recognized with the 2014 Nobel prize in Chemistry, revolutionized the field thanks to the possibility to achieve nanometric resolution, i.e., the typical scale length of chemical and biological phenomena. Since then, fluorescence microscopy-related techniques have acquired renewed interest for the scientific community, both from the perspective of instrument/techniques development and from the perspective of the advanced scientific applications. In this contribution we will review the application of these techniques to the field of drug delivery, discussing how the latest advancements of static and dynamic methodologies have tremendously expanded the experimental opportunities for the characterization of drug delivery systems and for the understanding of their behaviour in biologically relevant environments.

Download Full-text

Mechanisms and Pharmaceutical Action of Lipid Nanoformulation of Natural Bioactive Compounds as Efficient Delivery Systems in the Therapy of Osteoarthritis

Pharmaceutics ◽

10.3390/pharmaceutics13081108 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1108

Author(s):

Oana Craciunescu ◽

Madalina Icriverzi ◽

Paula Ecaterina Florian ◽

Anca Roseanu ◽

Mihaela Trif

Keyword(s):

Drug Delivery ◽

Bioactive Compounds ◽

Targeted Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Joint Disease ◽

Duration Of Action ◽

Immune System Activation

Osteoarthritis (OA) is a degenerative joint disease. An objective of the nanomedicine and drug delivery systems field is to design suitable pharmaceutical nanocarriers with controllable properties for drug delivery and site-specific targeting, in order to achieve greater efficacy and minimal toxicity, compared to the conventional drugs. The aim of this review is to present recent data on natural bioactive compounds with anti-inflammatory properties and efficacy in the treatment of OA, their formulation in lipid nanostructured carriers, mainly liposomes, as controlled release systems and the possibility to be intra-articularly (IA) administered. The literature regarding glycosaminoglycans, proteins, polyphenols and their ability to modify the cell response and mechanisms of action in different models of inflammation are reviewed. The advantages and limits of using lipid nanoformulations as drug delivery systems in OA treatment and the suitable route of administration are also discussed. Liposomes containing glycosaminoglycans presented good biocompatibility, lack of immune system activation, targeted delivery of bioactive compounds to the site of action, protection and efficiency of the encapsulated material, and prolonged duration of action, being highly recommended as controlled delivery systems in OA therapy through IA administration. Lipid nanoformulations of polyphenols were tested both in vivo and in vitro models that mimic OA conditions after IA or other routes of administration, recommending their clinical application.

Download Full-text

Rapid-Onset Sildenafil Sublingual Drug Delivery Systems: In Vitro Evaluation and In Vivo Pharmacokinetic Studies in Rabbits

Journal of Pharmaceutical Sciences ◽

10.1016/j.xphs.2016.01.015 ◽

2016 ◽

Vol 105 (9) ◽

pp. 2774-2781 ◽

Cited By ~ 7

Author(s):

Ming-Thau Sheu ◽

Chien-Ming Hsieh ◽

Ray-Neng Chen ◽

Po-Yu Chou ◽

Hsiu-O Ho

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Rapid Onset ◽

Delivery Systems ◽

Pharmacokinetic Studies ◽

In Vitro Evaluation

Download Full-text

Self-assembled drug delivery systems. Part 6: In vitro/in vivo studies of anticancer N-octadecanoyl gemcitabine nanoassemblies

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2012.03.046 ◽

2012 ◽

Vol 430 (1-2) ◽

pp. 276-281 ◽

Cited By ~ 18

Author(s):

Yiguang Jin ◽

Yanju Lian ◽

Lina Du ◽

Shuangmiao Wang ◽

Chang Su ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

In Vivo Studies ◽

Self Assembled

Download Full-text

Polymer-Based Smart Drug Delivery Systems for Skin Application and Demonstration of Stimuli-Responsiveness

Polymers ◽

10.3390/polym13081285 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1285

Author(s):

Louise Van Gheluwe ◽

Igor Chourpa ◽

Coline Gaigne ◽

Emilie Munnier

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Ex Vivo ◽

Delivery Systems ◽

Stimuli Responsive ◽

Stimuli Responsive Polymers ◽

Smart Drug ◽

Smart Drug Delivery

Progress in recent years in the field of stimuli-responsive polymers, whose properties change depending on the intensity of a signal, permitted an increase in smart drug delivery systems (SDDS). SDDS have attracted the attention of the scientific community because they can help meet two current challenges of the pharmaceutical industry: targeted drug delivery and personalized medicine. Controlled release of the active ingredient can be achieved through various stimuli, among which are temperature, pH, redox potential or even enzymes. SDDS, hitherto explored mainly in oncology, are now developed in the fields of dermatology and cosmetics. They are mostly hydrogels or nanosystems, and the most-used stimuli are pH and temperature. This review offers an overview of polymer-based SDDS developed to trigger the release of active ingredients intended to treat skin conditions or pathologies. The methods used to attest to stimuli-responsiveness in vitro, ex vivo and in vivo are discussed.

Download Full-text

Advances in Hybrid Polymer-Based Materials for Sustained Drug Release

International Journal of Polymer Science ◽

10.1155/2017/1231464 ◽

2017 ◽

Vol 2017 ◽

pp. 1-16 ◽

Cited By ~ 11

Author(s):

Lígia N. M. Ribeiro ◽

Ana C. S. Alcântara ◽

Gustavo H. Rodrigues da Silva ◽

Michelle Franz-Montan ◽

Silvia V. G. Nista ◽

...

Keyword(s):

Drug Delivery ◽

Drug Toxicity ◽

Drug Delivery Systems ◽

Hybrid Polymer ◽

Future Perspectives ◽

Sustained Drug Release ◽

Physicochemical Stability ◽

Traditional Drug

The use of biomaterials composed of organic pristine components has been successfully described in several purposes, such as tissue engineering and drug delivery. Drug delivery systems (DDS) have shown several advantages over traditional drug therapy, such as greater therapeutic efficacy, prolonged delivery profile, and reduced drug toxicity, as evidenced by in vitro and in vivo studies as well as clinical trials. Despite that, there is no perfect delivery carrier, and issues such as undesirable viscosity and physicochemical stability or inability to efficiently encapsulate hydrophilic/hydrophobic molecules still persist, limiting DDS applications. To overcome that, biohybrid systems, originating from the synergistic assembly of polymers and other organic materials such as proteins and lipids, have recently been described, yielding molecularly planned biohybrid systems that are able to optimize structures to easily interact with the targets. This work revised the biohybrid DDS clarifying their advantages, limitations, and future perspectives in an attempt to contribute to further research of innovative and safe biohybrid polymer-based system as biomaterials for the sustained release of active molecules.

Download Full-text

In vitro and in vivo techniques to assess the performance of gastro-retentive drug delivery systems: a review

Expert Opinion on Drug Delivery ◽

10.1517/17425247.5.9.951 ◽

2008 ◽

Vol 5 (9) ◽

pp. 951-965 ◽

Cited By ~ 14

Author(s):

Dhaivat C Parikh ◽

Avani F Amin

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Gastro Retentive

Download Full-text

Polymeric/Inorganic Multifunctional Nanoparticles for Simultaneous Drug Delivery and Visualization

MRS Proceedings ◽

10.1557/proc-1257-o04-03 ◽

2010 ◽

Vol 1257 ◽

Cited By ~ 2

Author(s):

Andrea Fornara ◽

Alberto Recalenda ◽

Jian Qin ◽

Abhilash Sugunan ◽

Fei Ye ◽

...

Keyword(s):

Drug Delivery ◽

Fluorescence Microscopy ◽

Contrast Agents ◽

Gold Nanorods ◽

In Vitro Cytotoxicity ◽

In Vivo Studies ◽

Multifunctional Nanoparticles ◽

Cytotoxicity Studies

AbstractNanoparticles consisting of different biocompatible materials are attracting a lot of interest in the biomedical area as useful tools for drug delivery, photo-therapy and contrast enhancement agents in MRI, fluorescence and confocal microscopy. This work mainly focuses on the synthesis of polymeric/inorganic multifunctional nanoparticles (PIMN) based on biocompatible di-block copolymer poly(L,L-lactide-co-ethylene glycol) (PLLA-PEG) via an emulsion-evaporation method. Besides containing a hydrophobic drug (Indomethacin), these polymeric nanoparticles incorporate different visualization agents such as superparamagnetic iron oxide nanoparticles (SPION) and fluorescent Quantum Dots (QDs) that are used as contrast agents for Magnetic Resonance Imaging (MRI) and fluorescence microscopy together. Gold Nanorods are also incorporated in such nanostructures to allow simultaneous visualization and photodynamic therapy. MRI studies are performed with different loading of SPION into PIMN, showing an enhancement in T2 contrast superior to commercial contrast agents. Core-shell QDs absorption and emission spectra are recorded before and after their loading into PIMN. With these polymeric/inorganic multifunctional nanoparticles, both MRI visualization and confocal fluorescence microscopy studies can be performed. Gold nanorods are also synthesized and incorporated into PIMN without changing their longitudinal absorption peak usable for lased excitation and phototherapy. In-vitro cytotoxicity studies have also been performed to confirm the low cytotoxicity of PIMN for further in-vivo studies.

Download Full-text

Natural Polysaccharides for siRNA Delivery: Nanocarriers Based on Chitosan, Hyaluronic Acid, and Their Derivatives

Molecules ◽

10.3390/molecules24142570 ◽

2019 ◽

Vol 24 (14) ◽

pp. 2570 ◽

Cited By ~ 14

Author(s):

Inés Serrano-Sevilla ◽

Álvaro Artiga ◽

Scott G. Mitchell ◽

Laura De Matteis ◽

Jesús M. de la Fuente

Keyword(s):

Drug Delivery ◽

Hyaluronic Acid ◽

Small Interfering Rna ◽

Drug Delivery Systems ◽

Sirna Delivery ◽

Delivery Systems ◽

Low Toxicity ◽

Interfering Rna

Natural polysaccharides are frequently used in the design of drug delivery systems due to their biocompatibility, biodegradability, and low toxicity. Moreover, they are diverse in structure, size, and charge, and their chemical functional groups can be easily modified to match the needs of the final application and mode of administration. This review focuses on polysaccharidic nanocarriers based on chitosan and hyaluronic acid for small interfering RNA (siRNA) delivery, which are highly positively and negatively charged, respectively. The key properties, strengths, and drawbacks of each polysaccharide are discussed. In addition, their use as efficient nanodelivery systems for gene silencing applications is put into context using the most recent examples from the literature. The latest advances in this field illustrate effectively how chitosan and hyaluronic acid can be modified or associated with other molecules in order to overcome their limitations to produce optimized siRNA delivery systems with promising in vitro and in vivo results.

Download Full-text