Article
Pharmacology & Pharmacy
Rosamaria Lombardo, Marika Ruponen, Jarkko Rautio, Carla Ghelardini, Lorenzo Di Cesare Mannelli, Laura Calosi, Daniele Bani, Riikka Lampinen, Katja M. Kanninen, Anne M. Koivisto, Elina Penttila, Heikki Lopponen, Rosario Pignatello
Summary: This study explored an alternative route of administration for clozapine (CZP) by encapsulating it in polymeric nanoparticles (NPs) for intranasal delivery. The NPs demonstrated controlled release and mucoadhesive properties, which could enhance the bioavailability of CZP.
Article
Nanoscience & Nanotechnology
Natalia N. Porfiryeva, Irina I. Semina, Ilgiz A. Salakhov, Rouslan I. Moustafine, Vitaliy V. Khutoryanskiy
Summary: Nasal drug delivery systems based on cationic and anionic Eudragit copolymers were designed, resulting in nanoparticles with mucoadhesive or mucus-penetrating properties for delivering haloperidol to the brain. Analysis on sheep nasal mucosa and rats in vivo confirmed the effectiveness of these nanoparticles in drug delivery.
NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE
(2021)
Article
Pharmacology & Pharmacy
Marketa Gajdosova, David Vetchy, Jan Muselik, Jan Gajdziok, Jan Jurica, Martina Vetcha, Karel Hauptman, Vladimir Jekl
Summary: The study developed bilayer mucoadhesive buccal films containing CPX for the treatment of oral candidiasis. Experimental results showed that CPX can accumulate in the oral mucosa tissue, which is beneficial for the treatment of oral candidiasis.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Biochemistry & Molecular Biology
Shahla Mirzaeei, Shiva Taghe, Raid G. Alany, Ali Nokhodchi
Summary: The present study aimed to enhance the delivery of erythromycin (ERY) by developing modified-release inserts containing ERY-loaded nanoparticles and mucoadhesive films. The developed inserts showed prolonged release profiles in vitro and in vivo, exhibited antibacterial efficacy, and did not cause irritation to the rabbit's eye. These findings suggest that nanoparticle-containing, mucoadhesive films could be a promising approach for topical ocular delivery of ERY.
Article
Pharmacology & Pharmacy
Anroop B. Nair, Jigar Shah, Shery Jacob, Bandar E. Al-Dhubiab, Vimal Patel, Nagaraja Sreeharsha, Pottathil Shinu
Summary: The study showed that optimizing mucoadhesive buccal films of rizatriptan can enhance its therapeutic efficacy for migraine treatment, with improved drug release and higher plasma levels compared to oral administration. This suggests that buccal films could be a promising alternative approach for effective rizatriptan delivery.
Article
Pharmacology & Pharmacy
Zhen Liang, Zhen Zhang, Ping Lu, Jingjing Yang, Lei Han, Susu Liu, Tianyang Zhou, Jingguo Li, Junjie Zhang
Summary: This study prepared modified solid lipid nanoparticles (SLNs) loaded with the antifungal drug econazole, showing that cationic SLNs exhibited improved antifungal activity, enhanced penetration ability, and sustained release compared to anionic SLNs.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Article
Pharmacology & Pharmacy
Ankita Goswami, Nirav Patel, Vaibhav Bhatt, Mihir Raval, Madhavi Kundariya, Navin Sheth
Summary: Currently, prostate cancer treatment has harmful side effects, so there is a need to develop safer treatments. This study developed a nanotechnology-based formulation loaded with carotenoid lycopene, which showed high encapsulation efficiency, optimum particle size, and good anti-prostate cancer potential.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Article
Pharmacology & Pharmacy
Shahla Mirzaeei, Shiva Taghe, Kofi Asare-Addo, Ali Nokhodchi
Summary: A novel nanofiber insert was prepared using modified electrospinning method to enhance ocular residence time of OFX with sustained release. The nanofibers were cross-linked and studied for OFX release through in vitro and in vivo methods, demonstrating antimicrobial efficacy and sustained drug release in ocular delivery systems.
Review
Pharmacology & Pharmacy
Aniket Nikam, Priya Ranjan Sahoo, Shubham Musale, Roshani R. Pagar, Ana Claudia Paiva-Santos, Prabhanjan Shridhar Giram
Summary: Eudragit, synthesized by radical polymerization, is a versatile polymer used for enteric coating, precise temporal release, and targeted delivery in the gastrointestinal system. Different grades of Eudragit are offered by Evonik Healthcare Germany, with the characteristics and potential applications determined by the ratio of methacrylic acid to its methacrylate-based monomers used in the polymerization reaction. Since 1953, Eudragit polymers have been widely used in healthcare applications worldwide. This review provides an overview of the current knowledge and gaps in understanding Eudragit, covering its molecular structure, material design, characterization, and healthcare applications.
Article
Nanoscience & Nanotechnology
Zhen Liang, Zhen Zhang, Jingjing Yang, Ping Lu, Tianyang Zhou, Jingguo Li, Junjie Zhang
Summary: The solid-lipid nanoparticle-based ECZ eye drops (E-SLNs) showed improved corneal permeability and antifungal activity without irritation compared to ECZ Suspension (E-Susp). E-SLNs exhibited controlled release and enhanced ocular bioavailability, making them a promising therapeutic approach for fungal keratitis and potentially other ocular diseases.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2021)
Article
Chemistry, Medicinal
Anwar Ma'ali, Hani Naseef, Moammal Qurt, Abdallah Damin Abukhalil, Abdullah K. Rabba, Israr Sabri
Summary: This research aimed to enhance the absorption of vitamin B-12 using sublingual mucoadhesive tablets. Formula S11 (Eudragit L100-55) was identified as the most favorable formulation with an optimal mucoadhesive residence time and drug release, suggesting an improved bioavailability of vitamin B-12 when this polymer is included.
Article
Pharmacology & Pharmacy
Saikat Pande, Janu Vashi, Ajay Solanki
Summary: This study investigated the potential of Eudragit coated chitosan microspheres in delivering Flurbiprofen in a sustained manner to the ileo-colonic region of the gastrointestinal tract for the treatment of ulcerative colitis. After optimization, the desired release profile was achieved, and the stability and molecular dispersion of the drug in the polymer matrix were confirmed.
CURRENT DRUG DELIVERY
(2022)
Article
Chemistry, Medicinal
Saniya Jawed, C. S. Satish
Summary: The study aims to develop a pulsatile and mucoadhesive drug delivery system for the time-regulated release of an ACE inhibitor Perindopril Erbumine to counteract early morning pathology like hypertension. Matrix tablets were prepared using Eudragit RSPO, Eudragit RLPO, and HPMC K15M. The optimized formulations P1T3 and P2T8 were coated for a lag time with compression coating of HPMC K4M and encapsulated in a Eudracap (TM) capsule to provide gastric resistance. The in-vitro release data showed a pause phase followed by a release of the drug to cope with the early morning rush in blood pressure, and a sustained release afterwards.
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
(2023)
Article
Polymer Science
Boglarka Szalai, Orsolya Jojart-Laczkovich, Anita Kovacs, Szilvia Berko, Gyorgy Tibor Balogh, Gabor Katona, Maria Budai-Szucs
Summary: This study aims to develop in situ gelling mucoadhesive ophthalmic preparations that can improve the bioavailability of eye drops. The results show that formulations based on thermosensitive polymers and mucoadhesive polymers can increase the residence time and penetration of the active pharmaceutical ingredient, thereby enhancing the bioavailability of the eye drops.
Article
Chemistry, Analytical
Chang Liu, Jianguo Dong, Zedong Zhang, Kexin Fu, Dekun Wang, Xue Mi, Shijing Yue, Xiaoyue Tan, Yuying Zhang
Summary: The physicochemical properties of nanoparticles significantly affect their accumulation at disease sites, thus impacting therapeutic efficacy. However, assessing the effects of different factors on nanoparticle accumulation within a single cell/tumor tissue is challenging due to a lack of appropriate labeling techniques. This study introduces a multiplexed SERS tracking approach to investigate the size-dependent accumulation and distribution of nanoparticles within the same tumor.
ANALYTICAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Lays Fernanda Nunes Dourado, Carolina Nunes da Silva, Rafael Silva Goncalves, Thomas Toshio Inoue, Maria Elena de Lima, Armando Da Silva Cunha-Junior
Summary: This study proposed the development of a drug nano-reservoir system, nanowafers containing PnPP-19, which demonstrated a hypotensive effect in rat's eyes when applied topically. The nanowafers showed prolonged release of the peptide compared to eye drops, and enhanced the hypotensive effect. These results suggest the potential therapeutic application of the nanowafers in treating retinal diseases such as glaucoma.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Review
Pharmacology & Pharmacy
Raquel Gregorio Arribada, Francine Behar-Cohen, Andre Luis Branco de Barros, Armando Silva-Cunha
Summary: The eye is constrained by anatomical and physiological barriers, limiting drug access. Polymer blends as drug delivery systems offer advantages but are not widely adopted.
Article
Pharmacology & Pharmacy
Julia Stephania Dos Reis, Aniely Dos Reis Teixeira, Amanda De Vasconcelos Quaresma, Tamires Cunha Almeida, Raquel Gregorio Arribada, Julia Teixeira Neto, Fabio Henrique Rodrigues Da Silva, Armando Silva-Cunha, Sandra Aparecida Lima De Moura, Glenda Nicioli Da Silva, Silvia Ligorio Fialho, Gisele Rodrigues Da Silva
Summary: The study found that sodium butyrate-loaded nanoparticles coated chitosan had a diameter of approximately 311.1 nm, a polydispersity index of 0.208, and a zeta potential of +56.3 mV; they were nontoxic to human retinal pigment epithelium cells, did not interfere with the integrity of rat's eye retinal layers, and inhibited angiogenesis in the chorioallantoic membrane assay.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2022)
Article
Chemistry, Multidisciplinary
Danielle Campiol Arruda, Anne-Marie Lachages, Helene Demory, Guillaume Escriou, Rene Lai-Kuen, Pierre-Yves Dugas, Celine Hoffmann, Stephanie Bessoles, Guillaume Sarrabayrouse, Angelo Malachias, Stephanie Finet, Pedro Lana Gastelois, Waldemar Augusto de Almeida Macedo, Armando da Silva Cunha, Pascal Bigey, Virginie Escriou
Summary: This study developed a novel lipid-polymer hybrid nanoparticle called Spheroplexes for efficient siRNA delivery. The nanoparticles consist of a hydrophobic PLGA matrix surrounded by a lipid envelope adopting a lamellar structure, in which the siRNA is complexed. The Spheroplexes were shown to be stable and more efficient than siRNA lipoplexes for delivering siRNA to cultured cells.
JOURNAL OF CONTROLLED RELEASE
(2022)
Article
Chemistry, Physical
Izabella E. de Carvalho, Brenda F. M. Castro, Lays F. N. Dourado, Carlos F. C. R. Guimaraes, Ivana S. Lula, Silvia L. Fialho, Armando da Silva Cunha Junior, Jarbas M. Resende, Elionai C. de L. Gomes
Summary: The study describes the synthesis and evaluation of peptide sequences and their carboxyamidated analogues as inhibitors of VEGF receptors involved in angiogenesis. Among them, PSAIWF-NH2 showed the highest inhibition of angiogenesis, comparable to bevacizumab. It has the advantage of not undergoing dimerization and can be obtained by a more efficient and cheaper synthetic method. In terms of cytotoxicity, all four peptides exhibited high cell viability in retinal cells.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Pharmacology & Pharmacy
Matheus Augusto de Castro, Pedro Henrique Reis, Christian Fernandes, Ricardo Geraldo de Sousa, Thomas Toshio Inoue, Silvia Ligorio Fiaiho, Armando Silva-Cunha
Summary: Ocular chemical burns can be effectively treated with a poloxamer-based thermoresponsive in-situ gelling system containing hyaluronic acid and indomethacin. The optimized system (F2) has a gelling temperature of 34.2 degrees C and shows improved wound healing in the ocular surface.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Nayara Almeida Lage, Mayara Rodrigues Brandao de Paiva, Daniel Vitor Vasconcelos-Santos, Renes Resende Machado, Silvia Ligorio Fialho, Armando Silva-Cunha
Summary: The study investigated the anti-inflammatory activity of Mometasone furoate (MF) in ocular tissues. It was found that at appropriate doses, MF was non-toxic and could attenuate disease progression, improve clinical, morphological, and functional parameters. The levels of inflammatory markers were also significantly reduced. Therefore, MF should be further explored as a promising drug for the treatment of ocular inflammation.
Article
Pharmacology & Pharmacy
Maria Carolina Andrade Guerra, Julia Teixeira Neto, Michele Gouvea Gomes, Lays Fernanda Nunes Dourado, Rodrigo Lambert Orefice, Luiz Guilherme Dias Heneine, Armando Silva-Cunha, Silvia Ligorio Fialho
Summary: Intravitreal injections are commonly used for drug delivery to the posterior segment of the eye, but their frequent administration leads to complications and poor adherence. Biodegradable nanofibers have the potential to regulate drug release and protect fragile bioactive drugs. Age-related macular degeneration is a leading cause of blindness and involves VEGF and inflammatory responses. In this study, we developed nanofiber-coated intravitreal implants for simultaneous delivery of dexamethasone and bevacizumab. The implants showed sustained drug release, reduction of vessels, and safety to the retina.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Cleildo P. Santana, Brock A. Matter, Madhoosudan A. Patil, Armando Silva-Cunha, Uday B. Kompella
Summary: This study aimed to determine corneal permeability and uptake in rabbit, porcine, and bovine corneas for twenty-five drugs and relate these parameters to drug physicochemical properties and tissue thickness through quantitative structure permeability relationships (QSPRs). The results showed that drug permeability was generally higher in rabbit cornea and comparable between bovine and porcine corneas. Corneal uptake between species correlated with a slope close to 1, indicating generally similar drug uptake per unit weight of tissue. The study also identified drug characteristics such as lipophilicity, heteroatom ratio, hydrogen bond acceptors, and tissue thickness that influence drug permeability and uptake.
Review
Oncology
Brenda F. M. Castro, Jason C. Steel, Christopher J. Layton
Summary: Age-related macular degeneration (AMD) and diabetic retinopathy (DR) are leading causes of blindness and vision loss worldwide. Current treatments for these diseases have limitations, and there is a need for alternative long-lasting options. Adeno-associated virus (AAV) has shown promise for ocular gene delivery, with studies exploring different strategies and pathways to optimize treatment. AAV-mediated gene delivery has shown promising results in preclinical and clinical trials for AMD and DR.
Review
Parasitology
Lutiana Amaral de Melo, Mayara Rodrigues Brandao de Paiva, Gabriella Maria Fernandes-Cunha, Armando Silva-Cunha, Marcos Paulo Gomes Mol, Silvia Ligorio Fialho
Summary: Based on a systematic review and meta-analysis, intravitreal injections were found to improve visual acuity and effectively treat ocular toxoplasmosis with minimal side effects. However, preexisting conditions should be carefully evaluated before making the decision to administer intravitreal injections.
REVISTA DA SOCIEDADE BRASILEIRA DE MEDICINA TROPICAL
(2023)
Article
Pharmacology & Pharmacy
Xueliang Xiu, Shichao Ma, Zhiyong Li, Zhipeng Li, Xuemei Li, Yangtao Ruan, Dezhao Li, Jianwei Wang, Fengsen Ma
Summary: Liposomes are promising delivery vehicles for drugs and vaccines. The use of microfluidic chips for liposome preparation is an effective method. However, traditional liposome preparation technologies hinder their industrial production and clinical application. This study presents a novel three-dimensional integrated microfluidic device for continuous liposome preparation and purification, which shows potential for industrial production of nano-pharmaceutical applications.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2024)
