Review
Pharmacology & Pharmacy
Hassan A. Albarqi, Anuj Garg, Mohammad Zaki Ahmad, Abdulsalam A. Alqahtani, Ismail A. Walbi, Javed Ahmad
Summary: Glaucoma is a chronic degenerative eye disease that leads to irreversible vision loss due to high intraocular pressure. Traditional ocular drug delivery systems have low bioavailability, making glaucoma therapy challenging. Chitosan-based nanoparticulate systems have shown promise in overcoming these limitations. This manuscript reviews recent research on chitosan-based nanoparticulate systems for glaucoma treatment, discussing their significance in improving drug residence time and ocular bioavailability. It also analyzes the impact of chitosan-based nanomedicine on corneal permeability, ocular bioavailability, and therapeutic performance of loaded antiglaucoma agents.
Review
Chemistry, Medicinal
Viliana Gugleva, Velichka Andonova
Summary: The challenge faced by researchers in achieving sufficient ocular bioavailability is due to the complex structure of the eye and its protective physiological mechanisms. Low viscosity eye drops and short ocular residence time contribute to low drug concentration at the target site. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are being developed as drug delivery platforms to overcome these challenges and enhance ocular bioavailability. They are biocompatible, biodegradable, and can be sterilized and scaled-up. Surface modifications can prolong ocular residence time, enhance penetration, and improve performance.
Review
Chemistry, Medicinal
Giuseppe Demarinis, Filippo Tatti, Andrea Taloni, Antonio Valentino Giugliano, Jesse Panthagani, James Myerscough, Enrico Peiretti, Giuseppe Giannaccare
Summary: Pregnancy requires cautious drug administration due to potential impacts on the fetus. Ophthalmologists need to consider the severity of the disease, individual treatment, routes of administration, and the latest safety information to optimize treatment outcomes and minimize risks.
Review
Pharmacology & Pharmacy
Andelka Racic, Danina Krajisnik
Summary: Dry eye syndrome and allergic conjunctivitis are common inflammatory disorders of the eye surface. The use of biopolymers in liquid ophthalmic preparations has advantages such as increasing tear film viscosity, exhibiting bioadhesive properties, and improving therapeutic effects. Methods for assessing mucoadhesiveness have been suggested, and this review provides an overview of the development of mucoadhesive liquid ophthalmic formulations for treating dry eye and allergic conditions.
Review
Pharmacology & Pharmacy
Bastien Leclercq, Dan Mejlachowicz, Francine Behar-Cohen
Summary: The eye is composed of tissues and cavities that are regulated to maintain their optical properties and functions. Specialized junctions between cells control the passage of drugs, while specific transporters regulate the movement of water, ions, and macromolecules. Ocular barriers limit the bioavailability of gene therapy products, but also allow for local treatment with minimal systemic side-effects. Understanding these barriers is essential for the development of efficient gene delivery systems.
Article
Biochemistry & Molecular Biology
Sarah Omran, Yosra S. R. Elnaggar, Ossama Y. Abdallah
Summary: A chitosan-coated luteolin-loaded phytocubosomal system was developed to enhance the therapeutic effects of luteolin in the treatment of glaucoma and ocular inflammation. This system showed nanosized particles with positive charge and improved drug encapsulation. It exhibited sustained drug release and improved anti-oxidant activity. The pharmacodynamic studies demonstrated significant reductions in intraocular pressure and faster recovery capabilities compared to other formulations.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2024)
Article
Pharmacology & Pharmacy
Dong-Jin Jang, Jun Hak Lee, Da Hun Kim, Jin-Woo Kim, Tae-Sung Koo, Kwan Hyung Cho
Summary: The purpose of this study was to develop clear aqueous rebamipide (REB) eye drops with improved solubility, stability, patient compliance, and bioavailability. The pH-modification method using NaOH and a hydrophilic polymer was employed to prepare a super-saturated 1.5% REB solution. The optimized eye drops formulation (F18 and F19) demonstrated long-term physicochemical stability and hypotonicity, and showed significantly long-lasting pharmacokinetic results in a rat study.
Review
Chemistry, Multidisciplinary
Cheng Peng, Liangju Kuang, Jiangyue Zhao, Amy E. Ross, Zhongqing Wang, Joseph B. Ciolino
Summary: This study conducted a bibliometric analysis on ocular drug delivery research over the past decade to characterize international trends and emerging frontiers. The results showed a significant increase in publications and citations, with the United States, the University of Florida, and Chauhan, Anuj being the most productive and impactful entities. The study identified important subtopics such as micro/nano ocular drug delivery systems, treatment of inflammation and posterior diseases, and emerging frontiers in ocular drug delivery.
JOURNAL OF CONTROLLED RELEASE
(2022)
Article
Biotechnology & Applied Microbiology
Aditya Josyula, Revaz Omiadze, Kunal Parikh, Pranjali Kanvinde, Matthew B. Appell, Pratikkumar Patel, Hiwa Saeed, Yogesh Sutar, Nicole Anders, Ping He, Peter J. McDonnell, Justin Hanes, Abhijit A. Date, Laura M. Ensign
Summary: This study describes an ion-pairing approach to creating MOX-PAM NS for the treatment of ocular infections, significantly increasing ocular drug absorption and demonstrating good prophylactic and treatment efficacy in a rat model.
BIOENGINEERING & TRANSLATIONAL MEDICINE
(2021)
Article
Veterinary Sciences
Lauren E. Page, Melissa A. Kubai, Rachel A. Allbaugh, Leila Bedos, Mackenzie M. Roy, Jonathan P. Mochel, Lionel Sebbag
Summary: The tear film kinetics can be determined by using different fluorescein concentrations and repeating eye drop administration at various time intervals. In this study, using 1% fluorescein solution showed higher tear film concentrations and a larger area-under-the-fluorescein-time curve compared to 0.3% solution. Repeating administration within 2-5 minutes after the first drop resulted in a significant increase in tear film concentrations for up to 20 minutes and the highest increase in the area-under-the-curve.
VETERINARY OPHTHALMOLOGY
(2023)
Article
Pharmacology & Pharmacy
Noriaki Nagai, Shunsuke Sakurai, Ryotaro Seiriki, Misa Minami, Mizuki Yamaguchi, Saori Deguchi, Eiji Harata
Summary: The MPC polymer prepared in this study showed hydrating effects without causing corneal damage, promoting tear film maintenance and improvement in dry eye symptoms.
Article
Pharmacology & Pharmacy
Lu Qin, Haiyang Wu, Enyu Xu, Xin Zhang, Jian Guan, Ruizhi Zhao, Shirui Mao
Summary: The study utilized functional polymer-lipid hybrid nanoparticles (PLHNs) to enhance oral absorption of BCS IV drugs, especially for those with poor solubility and permeability. Chitosan-modified PLHNs showed the strongest mucoadhesion among all tested formulations, with an absolute bioavailability of 21.95%. Incorporation of P-gp and CYP450 inhibitors further improved the oral bioavailability of the drug, with a 8-fold increase compared to the drug alone.
ASIAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Chemistry, Medicinal
Wenxiang Lin, Libei Zhao, Qian Tan, Ding Lin
Summary: The study showed that the combination of CTOIDD system with NVCM treatment effectively alleviated symptoms of severe acute bacterial S. aureus keratitis, with significantly better outcomes compared to eye drop NVCM and CTOIDD-saline groups.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2021)
Article
Materials Science, Multidisciplinary
Jeffrey Watchorn, Samantha Stuart, Darcy C. Burns, Frank X. Gu
Summary: Optimizing delivery vehicle properties is crucial for improving the delivery of pharmaceuticals. Mucoadhesion, a designed property that enhances the interaction between polymers and mucins, is an effective approach to increase drug residence times and uptake efficiency. Using nuclear magnetic resonance, this study investigated the influence of polymer design parameters on mucoadhesion and uncovered key findings on the polymer-mucin interaction at the atomic level. The results provide insights into the importance of polymer design and mucoadhesive functional groups for drug delivery.
ACS APPLIED POLYMER MATERIALS
(2022)
Article
Pharmacology & Pharmacy
Priyanka Agarwal, Johannes Korward, Sonja Krosser, Ilva D. Rupenthal
Summary: The addition of semifluorinated alkane and ethanol in eye drops can improve the penetration of Cyclosporine A (CsA) in the eyes, resulting in more efficient delivery to anterior ocular tissues compared to the commercial eyedrop, Ikervis. It reduces dose wastage and potential systemic side effects.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2023)
Article
Chemistry, Analytical
Andrea Cesari, Angela Fabiano, Anna Maria Piras, Ylenia Zambito, Gloria Uccello-Barretta, Federica Balzano
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2020)
Review
Biochemistry & Molecular Biology
Angela Fabiano, Denise Beconcini, Chiara Migone, Anna Maria Piras, Ylenia Zambito
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2020)
Article
Pharmacology & Pharmacy
Chiara Migone, Letizia Mattii, Martina Giannasi, Stefania Moscato, Andrea Cesari, Ylenia Zambito, Anna Maria Piras
Summary: The study aimed to develop a new vehicle for promoting the oral absorption of the neuropeptide DAL, which can cross both the intestinal mucosal barrier and blood-brain barrier. Results suggest the potential of DAL-NP in transporting a fraction of DAL dose administered orally to the brain, but further in vivo experiments are needed for confirmation.
Article
Chemistry, Medicinal
Anna Maria Piras, Ylenia Zambito, Maurizio Lugli, Baldassare Ferro, Paolo Roncucci, Filippo Mori, Alfonso Salvatore, Ester Ascione, Marta Bellini, Roberto Crea
Correction
Biochemistry & Molecular Biology
Anna Maria Piras, Semih Esin, Arianna Benedetti, Giuseppantonio Maisetta, Angela Fabiano, Ylenia Zambito, Giovanna Batoni
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Microbiology
Giuseppantonio Maisetta, Anna Maria Piras, Vincenzo Motta, Simona Braccini, Diletta Mazzantini, Federica Chiellini, Ylenia Zambito, Semih Esin, Giovanna Batoni
Summary: The low-molecular-weight quaternized chitosan derivative QAL demonstrates antivirulence activity against Pseudomonas aeruginosa by inhibiting the production of virulence factors and reducing swarming motility. Additionally, QAL shows the ability to regulate QS-related genes and inhibit bacterial growth synergistically with tobramycin.
Article
Biochemistry & Molecular Biology
Maria Michela Cesare, Francesca Felice, Veronica Conti, Luca Cerri, Ylenia Zambito, Marco Romi, Giampiero Cai, Claudio Cantini, Rossella Di Stefano
Summary: The study found that RED-Ds tomato peel extract has higher total polyphenol content compared to RED-Ctr, providing protection against oxidative stress and increasing antioxidant enzyme activity.
Article
Pharmacology & Pharmacy
Iryna Andrusenko, Victoria Hamilton, Arianna E. Lanza, Charlie L. Hall, Enrico Mugnaioli, Jason Potticary, Asma Buanz, Simon Gaisford, Anna M. Piras, Ylenia Zambito, Simon R. Hall, Mauro Gemmi
Summary: The structure of the 6-polymorph of indomethacin was determined using three-dimensional electron diffraction, showing enhanced dissolution rate and better biopharmaceutical properties. The knowledge of the structure allowed interpretation of spectroscopic data and observed a solid-solid transition from 6-polymorph to alpha-polymorph driven by molecular conformation similarities.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Pharmacology & Pharmacy
Angela Fabiano, Chiara Migone, Luca Cerri, Anna Maria Piras, Andrea Mezzetta, Giuseppantonio Maisetta, Semih Esin, Giovanna Batoni, Rossella Di Stefano, Ylenia Zambito
Summary: The study introduced olive leaves extract into microparticles for wound treatment, with blends of hyaluronic acid and chitosan in different proportions showing accelerated wound healing and good release effects.
Article
Biochemistry & Molecular Biology
Brunella Grassiri, Patrick Knoll, Angela Fabiano, Anna Maria Piras, Ylenia Zambito, Andreas Bernkop-Schnuerch
Summary: The goal of this study was to design and evaluate a thiolated cyclodextrin for ocular drug delivery, which provides high drug solubilizing and mucoadhesive properties. The results showed that thiolated cyclodextrin significantly enhanced the precorneal residence time and bioavailability of dexamethasone eye drops, making it suitable for ocular formulations of poorly soluble drugs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Angela Fabiano, Marinella De Leo, Luca Cerri, Anna Maria Piras, Alessandra Braca, Ylenia Zambito
Summary: This study successfully prepared self-assembling saffron extract nanoparticles with the assistance of chitosan, which protected crocin from degradation in simulated tear fluid and increased the residence time in the eyes.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Chiara Migone, Noemi Scacciati, Brunella Grassiri, Marinella De Leo, Alessandra Braca, Dario Puppi, Ylenia Zambito, Anna Maria Piras
Summary: Jellyfishes are considered as a potential resource in the food, pharmaceutical and biomedical industries. In this study, jellyfish skin polysaccharides (JSP) with glycosaminoglycan (GAG) features were extracted and evaluated for their potential as wound healing promoters and antioxidants. The results showed that the JSPs were effective in promoting scratch repair and protecting cells from oxidative stress. These GAG-like polysaccharides have potential applications in biomedical skin treatments and as pharmaceutical excipients.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Emily Cioni, Chiara Migone, Roberta Ascrizzi, Beatrice Muscatello, Marinella De Leo, Anna Maria Piras, Ylenia Zambito, Guido Flamini, Luisa Pistelli
Summary: Comparative chemical analyses of peel and pulp extracts from different varieties of Citrus australasica showed variations in composition and antioxidant activity. Collette peel and Pink Ice pulp were rich in flavonoids, while Collette and Red peel exhibited the highest activity in protecting against oxidative damage.
Article
Biochemistry & Molecular Biology
Brunella Grassiri, Andrea Mezzetta, Giuseppantionio Maisetta, Chiara Migone, Angela Fabiano, Semih Esin, Lorenzo Guazzelli, Ylenia Zambito, Giovanna Batoni, Anna Maria Piras
Summary: The study evaluated the use of ionic liquids (ILs) as functional excipients for solubilizing and stabilizing diacerein (DIA) in eye drop formulations and prolonging its ocular residence time. Two ILs based on natural zwitterionic compounds were investigated: L-carnitine C6 alkyl ester bromide (Carn6) and betaine C6 alkyl ester bromide (Bet6). The ILs demonstrated solubilizing, stabilizing, mucoadhesive, and antimicrobial properties, with potential for future use in ophthalmic applications.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Food Science & Technology
Ylenia Zambito, Anna Maria Piras, Angela Fabiano
Summary: In this study, a conjugate based on a quaternary ammonium chitosan derivative and methyl-beta CD was prepared to encapsulate bergamot essential oil (BEO). The conjugate was able to stabilize the volatile compounds of BEO and convert it into a solid dosage form. The obtained conjugate showed good solubility and high extract association efficiency of polyphenols and limonene. The stability studies demonstrated that the conjugate was effective in protecting polyphenols and limonene from degradation under UV stress. The transformation of the liquid oil into a solid dosage form eliminated the unpleasant taste and improved the bioavailability.
Article
Pharmacology & Pharmacy
Greta Camilla Magnano, Marika Quadri, Elisabetta Palazzo, Roberta Lotti, Francesca Loschi, Stefano Dall'Acqua, Michela Abrami, Francesca Larese Filon, Alessandra Marconi, Dritan Hasa
Summary: This study aimed to investigate the loading of sildenafil citrate in three commercial transdermal vehicles using 3D full-thickness skin equivalent and compare the results with permeability experiments using porcine skin. The results showed that the results obtained using the 3D skin equivalent were comparable to those obtained using porcine skin, suggesting that the 3D skin model can be a valid alternative for ex-vivo skin absorption experiments.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2024)
Article
Pharmacology & Pharmacy
James W. Mckeage, Andrew Z. H. Tan, Andrew J. Taberner
Summary: Needle-free jet injection is a promising alternative drug delivery technique that offers rapid, non-invasive, and large-volume injections. The study presents a prototype multi-orifice nozzle and a computational fluid dynamic model to demonstrate the feasibility and effectiveness of this technology.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2024)