Article
Instruments & Instrumentation
Jorge Jimenez, Michael A. Washington, Jayde L. Resnick, Ken K. Nischal, Morgan Fedorchak
Summary: This study presents a novel controlled release eyedrop formulation of cysteamine to address the dosing frequency and stability issues faced by patients with cystinosis when using traditional eyedrops. The controlled release system showed improved stability, reduced dosing frequency, and enhanced ocular penetration compared to aqueous cysteamine eyedrops. In vivo and in vitro studies demonstrated good tolerability and retention of the drug, suggesting that this once daily gel eyedrop may offer a stable delivery of cysteamine for patients.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2021)
Review
Pharmacology & Pharmacy
Liping Li, Fan Jia, Youxiang Wang, Jiamin Liu, Yi Tian, Xinghuai Sun, Yuan Lei, Jian Ji
Summary: This review focuses on recent advancements in using nanomaterials for efficient drug transport across the cornea, categorizing and analyzing their mechanisms, and examining potential principles to improve drug penetration through the cornea and other natural barriers in the eye. The aim is to inspire the development of more effective drug delivery systems for better treatment of ocular diseases.
ADVANCED DRUG DELIVERY REVIEWS
(2023)
Review
Ophthalmology
Sukhmandeep Kaur, Phulen Sarma, Hardeep Kaur, Manisha Prajapat, Nishant Shekhar, Jaimini Bhattacharyya, Harpinder Kaur, Subodh Kumar, Bikash Medhi, Jagat Ram, Dipankar Das, Pramod Avti, Ajay Prakash, Rahul Singh, Anusuya Bhattacharyya
Summary: This study found that cysteamine performed better than placebo and control in terms of treatment response and improvement, and was more effective in reducing corneal cystine density compared to other formulations.
AMERICAN JOURNAL OF OPHTHALMOLOGY
(2021)
Article
Ophthalmology
Charis B. Hoppe, Sean Yonamine, Brandon W. Kao, Marcus L. Turner, Yvonne Ou, Ying Han, Jeremy D. Keenan, Julius T. Oatts
Summary: This study evaluated the noninferiority of a small-volume eye drop adapter, the Nanodropper, compared to the standard of care in terms of pupillary dilation and cycloplegia in children. The results showed that the efficacy of the small-volume eye drops was comparable to the standard treatment, indicating the potential to reduce medical waste and medication toxicity.
Article
Medicine, General & Internal
Csorba Anita, Maka Erika, Szabo Attila, Kelen Kata, Reusz Gyorgy, Nagy Zoltan Zsolt
Summary: This study reviewed the ocular clinical manifestations and treatment options of cystinosis, and presented the first clinical application of viscous cysteamine eye drops in a cystinosis patient in Hungary. The results showed that the use of viscous cysteamine eye drops significantly reduced photophobia and decreased corneal crystal density.
Review
Chemistry, Inorganic & Nuclear
Qiuxiang Wang, Aiwen Zhang, Lu Zhu, Xuewen Yang, Guihua Fang, Bo Tang
Summary: Cyclodextrin (CD), a cyclic oligosaccharide, is a promising pharmaceutical excipient due to its ability to form complexes with small molecules and polymers. Over the past two decades, CD-based ocular drug delivery systems have rapidly developed, offering excellent biocompatibility, safety, and stability. This review discusses recent progress in CD-based ocular drug delivery systems, including drug/CD complexes, CD-based nanocarriers and microcarriers, CD-based hydrogels, and CD-based inserts. Additionally, the methods for ocular safety evaluation and patents and clinical trials for CD-based ocular drug delivery systems are systematically summarized.
COORDINATION CHEMISTRY REVIEWS
(2023)
Article
Chemistry, Multidisciplinary
Hui Shi, Jianhong Zhou, Yuan Wang, Yutuo Zhu, Deqing Lin, Lei Lei, Serhii Vakal, Jiaqing Wang, Xingyi Li
Summary: This study presents a minimally invasive delivery system for treating fungal keratitis using a dissolving microneedle patch based on Poly(D,L-lactide) and hyaluronic acid. The microneedle patch shows excellent properties and can penetrate the cornea with no ocular irritation. In a rabbit model, the microneedle patch medication exhibits superior therapeutic effects compared to eye drops and is comparable to intrastromal injection, offering a cost-effective treatment solution.
Review
Pharmacology & Pharmacy
Phatsawee Jansook, Thorsteinn Loftsson
Summary: Cyclodextrins, particularly gamma-cyclodextrin, have been extensively used in pharmaceutical products to improve the solubility and bioavailability of drugs. They can self-assemble to form nano- and microparticles, increasing drug solubility and permeability. Clinical studies have shown their potential in enhancing drug delivery to the eye.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Review
Pharmacology & Pharmacy
Blanca Lorenzo-Veiga, Carmen Alvarez-Lorenzo, Thorsteinn Loftsson, Hakon Hrafn Sigurdsson
Summary: Age-related eye disorders are a major global health concern, with challenges in drug targeting and treatment effectiveness. Conventional treatments have limitations, while new drug delivery systems and medical devices are being developed but may not always be effective.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Materials Science, Multidisciplinary
Qiaoyun Gong, Yue Zhao, Tianwei Qian, Haiyan Wang, Zuhao Li
Summary: Functionalized hydrogels show great potential in ophthalmic applications. This review summarizes the various functionalized hydrogels for different eye diseases and introduces advanced research progress in ophthalmic applications. Engineered hydrogels are expected to become powerful tools for the treatment of ocular diseases in the future.
MATERIALS & DESIGN
(2022)
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
Carlo Astarita, Sara Palchetti, Mina Massaro-Giordano, Marina Di Domenico, Francesco Petrillo, Silvia Boffo, Giulio Caracciolo, Antonio Giordano
Summary: Topical administration is a convenient route for ocular drug delivery, but only a small fraction of the drug is retained in the precorneal pocket. The protein corona (PC) formed around drug delivery systems (DDS) changes their properties, affecting their interaction with ocular cells. Coating lipoplexes with artificial PCs enhances their internalization in corneal epithelial cells, showing potential for targeted ocular drug delivery.
Article
Nanoscience & Nanotechnology
Chenchen Zhang, Yuan Yin, Jing Zhao, Yanxia Li, Yuanping Wang, Zhaoying Zhang, Lingzhi Niu, Yajuan Zheng
Summary: CNV is an ocular pathological change caused by various ocular insults. Current treatment strategies for CNV have limitations. Gene-based and nanotechnology-based therapies have shown promising results. This review provides an overview of CNV treatment strategies and summarizes the properties and applications of various nanosystems in the field.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2022)
Article
Biochemistry & Molecular Biology
Rakesh Swain, Souvik Nandi, Shasank Sekhar Swain, Krushna Prasad Pattanaik, Sujata Mohapatra, Dhananjay Panigrahi, Subrata Mallick
Summary: Bentonite is used for safe and controlled ocular drug delivery. A sol-to-gel formulation consisting of hydroxypropyl methylcellulose (HPMC) and poloxamer combined with bentonite has been developed for the prophylactic ocular anti-inflammatory effect of trimetazidine. The sol formulation showed good tolerability and sustained release and permeation profiles, resulting in a stable and sustained effect. The HPMC-poloxamer-based in-situ gel with bentonite can be utilized for sustained ocular delivery and inflammation control.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Pharmacology & Pharmacy
Andrea Conde Penedo, Victoria Diaz Tome, Anxo Fernez Ferreiro, Miguel Gonzalez Barcia, Francisco J. Otero Espinar
Summary: The study confirmed the potential value of various formulations for transepithelial crosslinking in keratoconus patients, by increasing riboflavin permeability and enhancing drug solubility, without observed irritation or adverse effects on the eyes.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2021)
Article
Engineering, Chemical
Rayanne R. Pereira, Antonio T. A. Gomes, Matteo Testi, Annalisa Bianchera, Roseane M. Ribeiro-Costa, Cristina Padula, Jose O. C. Silva Junior, Fabio Sonvico
Summary: Experimental design and data analysis demonstrated that increasing pressure and homogenization cycles contribute to reducing the mean particle size and PDI of NLCs, but only when TPGS is present as the surfactant.
CHEMICAL ENGINEERING & TECHNOLOGY
(2021)
Article
Biochemical Research Methods
Anna Demurtas, Silvia Pescina, Sara Nicoli, Patrizia Santi, Daniele Ribeiro de Araujo, Cristina Padula
Summary: A simple and sensitive HPLC method was developed for the quantification of budesonide in skin layers. The method showed good selectivity, wide linear range, high precision and accuracy, and was found to be suitable for quantification of budesonide in skin layers at the end of in vitro permeation experiments.
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
(2021)
Review
Chemistry, Multidisciplinary
M. Ghezzi, S. Pescina, C. Padula, P. Santi, E. Del Favero, L. Cantu, S. Nicoli
Summary: Polymeric micelles, innovative aggregation colloids formed by self-assembling of amphiphilic polymers in solution, offer advantages in drug administration but also face challenges such as lower stability and complex characterization. Understanding their interaction with the biological environment is crucial, and a combination of different characterization techniques can provide a deeper insight into their in vivo behavior.
JOURNAL OF CONTROLLED RELEASE
(2021)
Review
Pharmacology & Pharmacy
Felipe M. Gonzalez-Fernandez, Annalisa Bianchera, Paolo Gasco, Sara Nicoli, Silvia Pescina
Summary: Nanotherapeutics based on biocompatible lipid matrices enhance the solubility of poorly soluble compounds in treating ophthalmic diseases by utilizing micro-/nanoemulsions, solid lipid nanoparticles (SLN) or nanostructured lipid carriers (NLC). These lipid-based drug delivery systems improve drug stability and ocular bioavailability, with the potential to optimize drug delivery platforms and reduce research costs through quality-by-design (QbD) and design-of-experiments (DoE) approaches.
Article
Pharmacology & Pharmacy
Martina Ghezzi, Silvia Pescina, Andrea Delledonne, Ilaria Ferraboschi, Cristina Sissa, Francesca Terenziani, Paula De Freitas Rosa Remiro, Patrizia Santi, Sara Nicoli
Summary: The study aimed to improve the solubility and skin retention of Imiquimod using micelles of TPGS and oleic acid, which showed significant enhancement in drug solubility and micellar stability. The delivery efficiency of this formulation was found to be 42- and 25-folds higher than that of commercial creams after application.
Article
Pharmacology & Pharmacy
Silvia Pescina, Fabio Sonvico, Adryana Clementino, Cristina Padula, Patrizia Santi, Sara Nicoli
Summary: There is a growing consensus on the beneficial effects of statins for age-related macular degeneration and inflammatory diseases affecting the posterior segment of the eye. The development of polymeric micelles has shown promising results in improving the solubility and stability of simvastatin, with the potential for enhanced drug delivery to the posterior segment of the eye. This research paves the way for future viable ocular administration of statins.
Article
Biochemical Research Methods
Luca Giulio, Cristina Padula, Silvia Pescina, Sara Nicoli, Patrizia Santi
Summary: An innovative and sensitive HPLC-UV method was developed and validated for the extraction and quantification of methotrexate in skin layers. The method is suitable and accurate.
BIOMEDICAL CHROMATOGRAPHY
(2022)
Article
Pharmacology & Pharmacy
Paula de Freitas Rosa Remiro, Mariana Harue Taniguchi Nagahara, Martina Ghezzi, Alessia Filippini, Anna Demurtas, Silvia Pescina, Patrizia Santi, Cristina Padula, Angela Maria Moraes, Sara Nicoli
Summary: This study developed buccal formulations for topical administration of imiquimod, aiming to improve mucosal retention and reduce trans-mucosal permeation compared to the reference formulation. The developed hydrogels and films showed comparable in vitro performance to the commercial formulation, with significantly reduced permeation in the case of the xanthan gum film.
Article
Pharmacology & Pharmacy
Felipe M. Gonzalez-Fernandez, Andrea Delledonne, Sara Nicoli, Paolo Gasco, Cristina Padula, Patrizia Santi, Cristina Sissa, Silvia Pescina
Summary: This research aims to develop nanostructured lipid carriers (NLC) for periocular administration of dexamethasone acetate for the treatment of ocular inflammation. The NLC was formulated using solid and liquid lipid mixtures, resulting in a particle size of 106.9 +/- 1.2 nm, PDI = 0.104 +/- 0.019, and zeta potential = -6.51 +/- 0.575 mV. Ex vivo permeation studies showed that dexamethasone acetate was metabolized into free dexamethasone and exhibited higher permeation capabilities across both sclera and choroid tissues.
Article
Pharmacology & Pharmacy
Adriana Fantini, Luca Giulio, Andrea Delledonne, Silvia Pescina, Cristina Sissa, Sara Nicoli, Patrizia Santi, Cristina Padula
Summary: The optimization of non-invasive formulations for the delivery of high molecular weight compounds is the greatest achievement in the field of advanced drug delivery. Permeation experiments using fatty acids and bile salts as penetration enhancers showed that it is feasible to increase the mucosa permeation of high molecular weight dextrans. This study suggests that buccal administration can be used for the delivery of high molecular weight compounds.