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https://www.readbyqxmd.com/read/28986195/surface-modified-mucoadhesive-microgels-as-a-controlled-release-system-for-miconazole-nitrate-to-improve-localized-treatment-of-vulvovaginal-candidiasis
#1
Franklin C Kenechukwu, Anthony A Attama, Emmanuel C Ibezim, Petra O Nnamani, Chukwuebuka E Umeyor, Emmanuel M Uronnachi, Thaddeus H Gugu, Mumuni A Momoh, Kenneth C Ofokansi, Paul A Akpa
The use of conventional vaginal formulations of miconazole nitrate (MN) in the treatment of deep-seated VVC (vulvovaginal candidiasis) is limited by poor penetration capacity and low solubility of MN, short residence time and irritation at the application site. Surface-modified mucoadhesive microgels were developed to minimize local irritation, enhance penetration capacity and solubility and prolong localized vaginal delivery of MN for effective treatment of deep-seated VVC. Solid lipid microparticles (SLMs) were prepared from matrices consisting of hydrogenated palm oil (Softisan® 154, SF) and super-refined sunseed oil (SO) with or without polyethylene glycol (PEG)-4000, characterized for physicochemical performance and used to prepare mucoadhesive microgels (MMs) encapsulating MN, employing Polycarbophil as bioadhesive polymer...
October 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28971375/in-vitro-and-in-vivo-studies-on-a-novel-bioadhesive-colloidal-system-cationic-liposomes-of-ibuprofen
#2
Xiumei Gai, Lizhen Cheng, Ting Li, Dandan Liu, Yanyan Wang, Tuanjie Wang, Weisan Pan, Xinggang Yang
The objective of this study was to develop an ocular drug delivery system built on the cationic liposomes, a novel bioadhesive colloidal system, which could enhance the precorneal residence time, ocular permeation, and bioavailability of ibuprofen. The optimal formulation of cationic liposomes prepared by ethanol injection method was ultimately confirmed by an orthogonal L9 (3(3)) test design. In addition, γ-scintigraphic technology and the microdialysis technique were utilized in the assessment of in vivo precorneal retention capability and ocular bioavailability individually...
October 2, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28964952/preparation-and-characterization-of-intravaginal-vardenafil-suppositories-targeting-a-complementary-treatment-to-boost-in-vitro-fertilization-process
#3
Eman Gomaa, Amr S Abu Lila, Azza A Hasan, Fakhr-Eldin S Ghazy
Vaginal route has been recently considered as a potential route for systemic delivery of drugs with poor oral bioavailability. Vardenafil (VDF) is a relatively new phosphodiesterase-5 inhibitor that exhibits a limited oral bioavailability (≈15%) due to extensive first-pass metabolism. In this study, we attempted to enhance the systemic bioavailability of VDF via its formulation within vaginal suppositories. Witepsol H15 and Suppocire NA50 were adopted as lipophilic suppository bases while polyethylene glycol 4000/400 and glycerogelatin were used as hydrophilic suppository bases...
September 28, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28945033/-preparation-and-evaluation-of-gastric-adhesive-floating-pellets-for-bolo-leaf-phenols
#4
Ya-Li He, Ying Li, Dan-Dan Yang, Chun-Yan Zhu
Gastric adhesive-floating pellets for Bolo leaf phenols (BLP) were prepared by extrusion-spheronization method, with chitosan as skeleton bioadhesive material, and stearyl alcohol as help-bleaching agent to evaluate its in vitro adhesivity, floatability and in vivo retention situation, and investigate its in vitro release characteristics. The in vitro adhesivity and floatability were evaluated respectively by in vitro tissue retention method and visual observation method. The retention of pellets in rats was investigated by in vivo tissue retention method and in vivo imaging of small animals...
January 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28945014/a-reloadable-self-healing-hydrogel-enabling-diffusive-transport-of-c-dots-across-gel-gel-interface-for-scavenging-reactive-oxygen-species
#5
Jing Chen, Shuya Li, Ye Zhang, Wei Wang, Xiang Zhang, Yangyang Zhao, Yucai Wang, Hong Bi
While reloadable drug delivery platforms are highly prized for the treatment of a broad spectrum of diseases, the gel-gel interface between hydrogels hinders the intergel diffusive transport of drugs and thus limits the application of hydrogels as reloadable depots. Here, this study reports the circumvention of this barrier by employing a self-healing hydrogel prepared from N-carboxyethyl chitosan and sodium alginate dialdehyde, which are cross-linked via a reversible Schiff base linkage. The injectable and bioadhesive hydrogel shows a rapid gelation time of 47 s...
September 25, 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/28943206/kaolinite-in-pharmaceutics-and-biomedicine
#6
REVIEW
Mahmoud E Awad, Alberto López-Galindo, Massimo Setti, Mahmoud M El-Rahmany, César Viseras Iborra
Kaolinite Al2Si2O5(OH)4 is an abundant and inexpensive geomaterial regarded as one of the most common clay minerals in the earth's crust and the most widespread phase among the other kaolin polymorphs (halloysite, dickite and nacrite). Structurally, it is a hydrous aluminum phyllosilicate member belonging to the dioctahedral 1:1 kaolin mineral group. The particle size of the pseudohexagonal kaolinite platelets is normally <2μm (if compared to a human red blood cell of a typical diameter 6.2-8.2μm or to a virus particle of about 50nm diameter)...
September 22, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28920559/functional-mechanics-of-a-pectin-based-pleural-sealant-after-lung-injury
#7
Andrew B Servais, Cristian D Valenzuela, Arne Kienzle, Alexandra B Ysasi, Willi L Wagner, Akira Tsuda, Maximilian Ackermann, Steven J Mentzer
Pleural injury and associated air leaks are a major influence on patient morbidity and health care costs after lung surgery. Pectin, a plant-derived heteropolysaccharide, has recently demonstrated potential as an adhesive binding to the glycocalyx of visceral mesothelium. Since bioadhesion is a process likely involving the interpenetration of the pectin-based polymer with the glycocalyx, we predicted that the pectin-based polymer may also be an effective sealant for pleural injury. To explore the potential role of an equal weight % mixture of high-methoxyl pectin and carboxymethylcellulose as a pleural sealant, we compared the yield strength of the pectin-based polymer to commonly available surgical products...
September 16, 2017: Tissue Engineering. Part A
https://www.readbyqxmd.com/read/28917926/bioadhesive-and-biocompatible-films-as-wound-dressing-materials-based-on-a-novel-dendronized-chitosan-loaded-with-ciprofloxacin
#8
Mónica C García, Ana A Aldana, Luis I Tártara, Fabiana Alovero, Miriam C Strumia, Rubén H Manzo, Marisa Martinelli, Alvaro F Jimenez-Kairuz
The bioadhesive polymeric films as topical drug delivery systems are interesting alternatives to improve the pharmacotherapy and patient compliances. New derivate biomaterials based on weisocyanate- dendronized PVP- crosslinked chitosan and loaded with ciprofloxacin (CIP), as model drug, were used to prepare bioadhesive films. Relevant in vitro/in vivo attributes to define main physicochemical and biopharmaceutical characteristics for topical wound-healing applications were evaluated. A high proportion of CIP, uniformly dispersed along throughout the film, was loaded...
November 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28900598/cationic-pegylated-polycaprolactone-nanoparticles-carrying-post-operation-docetaxel-for-glioma-treatment
#9
Cem Varan, Erem Bilensoy
Background: Brain tumors are the most common tumors among adolescents. Although some chemotherapeutics are known to be effective against brain tumors based on cell culture studies, the same effect is not observed in clinical trials. For this reason, the development of drug delivery systems is important to treat brain tumors and prevent tumor recurrence. The aim of this study was to develop core-shell polymeric nanoparticles with positive charge by employing a chitosan coating. Additionally, an implantable formulation for the chemotherapeutic nanoparticles was developed as a bioadhesive film to be applied at the tumor site following surgical operation for brain glioma treatment...
2017: Beilstein Journal of Nanotechnology
https://www.readbyqxmd.com/read/28892400/poly-vinyl-methyl-ether-maleic-anhydride-doped-peg-pla-nanoparticles-for-oral-paclitaxel-delivery-to-improve-bioadhesive-efficiency
#10
Qian Wang, Chan Li, Tianyang Ren, Shizhu Chen, Xiaoxia Ye, Hongbo Guo, Haibing He, Yu Zhang, Tian Yin, Xing-Jie Liang, Xing Tang
Bioadhesive nanoparticles based on poly(vinyl methyl ether/maleic anhydride) (PVMMA) and poly(ethylene glycol) methyl ether-b-poly(d,l-lactic acid) (mPEG-b-PLA) were produced by the emulsification solvent evaporation method. Paclitaxel was utilized as the model drug, with an encapsulation efficiency of up to 90.2 ± 4.0%. The nanoparticles were uniform and spherical in shape and exhibited a sustained drug release compared with Taxol. m-NPs also exhibited favorable bioadhesive efficiency at the same time. Coumarin 6 or DiR-loaded nanoparticles with/without PVMMA (C6-m-NPs/DiR-m-NPs or C6-p-NPs/DiR-p-NPs) were used for cellular uptake and intestinal adhesion experiments, respectively...
October 2, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28887234/vaginal-semisolid-products-technological-performance-considering-physiologic-parameters
#11
Rita Monteiro Machado, Ana Palmeira-de-Oliveira, José Martinez-de-Oliveira, Rita Palmeira-de-Oliveira
Vaginal semisolid products are frequently used to treat vaginal infections and atrophy-related symptoms of menopause. Formulations composition and the methods for their characterization, especially those developed concerning the target epithelia, are key tools to predict in vivo results at early stages of product development. However, recent studies on this subject have been almost exclusively focused on anti-HIV preparations. The aim of this work consists on improving traditional characterization methods by using physiological parameters in order to construct predictive tools to characterize a new ideal vaginal semisolid formulation whatever target it may have...
September 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28866150/synthesis-and-study-of-thermal-mechanical-and-biodegradation-properties-of-chitosan-g-pmma-with-chicken-egg-shell-nano-cao-as-a-novel-bio-filler
#12
Arun K Pradhan, Prafulla K Sahoo
The important objective of this study is to evaluate the effect of chicken eggshell (nano-Cao) as a functionalized bio-filler on the mechanical strength and thermal stability of acrylic based bionanocomposite of chitosan grafted with poly(methyl methacrylate)(PMMA). The chitosan grafted PMMA adsorbed with functionalized biofiller was prepared via emulsion polymerisation technique and physicochemically characterized as bone graft substitute. The so prepared grafted bioactive bone cement (BBC) bionanocomposite (BNC), chitosan-g-PMMA/nano-CaO was characterized by FTIR, XRD, FESEM and TGA...
November 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28853566/tunicate-inspired-gallol-polymers-for-underwater-adhesive-a-comparative-study-of-catechol-and-gallol
#13
Kan Zhan, Chaehoon Kim, Kyungmo Sung, Hirotaka Ejima, Naoko Yoshie
Man-made glues often fail to stick in wet environments because of hydration-induced softening and dissolution. The wound healing process of a tunicate inspired the synthesis of gallol-functionalized copolymers as underwater adhesive. Copolymers bearing three types of phenolic groups, namely, phenol, catechol, and gallol, were synthesized via the methoxymethyl protection/deprotection route. Surprisingly, the newly synthesized copolymers bearing gallol groups exhibited stronger adhesive performances (typically 7× stronger in water) than the widely used catechol-functionalized copolymers under all tested conditions (in air, water, seawater, or phosphate-buffered saline solution)...
August 30, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28829952/degradable-bioadhesive-nanoparticles-for-prolonged-intravaginal-delivery-and-retention-of-elvitegravir
#14
Muneeb Mohideen, Elias Quijano, Eric Song, Yang Deng, Gauri Panse, Wei Zhang, Meredith R Clark, W Mark Saltzman
New methods for long-lasting protection against sexually transmitted disease, such as the human immunodeficiency virus (HIV), are needed to help reduce the severity of STD epidemics, especially in developing countries. Intravaginal delivery of therapeutics has emerged as a promising strategy to provide women with local protection, but residence times of such agents are greatly reduced by the protective mucus layer, fluctuating hormone cycle, and complex anatomical structure of the reproductive tract. Polymeric nanoparticles (NPs) capable of encapsulating the desired cargo, penetrating through the mucosal surfaces, and delivering agents to the site of action have been explored...
November 2017: Biomaterials
https://www.readbyqxmd.com/read/28822703/turning-the-screw-even-further-to-increase-microparticle-retention-and-ocular-bioavailability-of-associated-drugs-the-bioadhesion-goal
#15
J Rodríguez Villanueva, L Rodríguez Villanueva
Ocular drug delivery is one of the most fascinating and challenging tasks facing pharmaceutical researchers. Improving drug ocular residence time and/or penetration is complex. Microparticles (MP) provide interesting opportunities to increase ocular bioavailability of drugs and patient compliance brought about by decreased frequency of dosing. However, sustained-release microsphere formulation would fail to accomplish the task of long-lasting drug release unless microspheres remained for a prolonged period at the site of action...
August 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28809108/dual-regulations-of-thermosensitive-heparin-poloxamer-hydrogel-using-%C3%AE%C2%B5-polylysine-bioadhesivity-and-controlled-kgf-release-for-enhancing-wound-healing-of-endometrial-injury
#16
He-Lin Xu, Jie Xu, Bi-Xin Shen, Si-Si Zhang, Bing-Hui Jin, Qun-Yan Zhu, De-Li ZhuGe, Xue-Qing Wu, Jian Xiao, Ying-Zheng Zhao
Hydrogel was not only used as an effective support matrix to prevent intrauterine adhesion after endometrial injury but also served as scaffold to sustain release of some therapeutics, especially growth factor. However, because of the rapid turnover of the endometrial mucus, the poor retention and bad absorption of therapeutic agents in damaged endometrial cavity were two important factors hindering their pharmacologic effect. Herein, a mucoadhesive hydrogel was described by using heparin-modified poloxamer (HP) as the matrix material and ε-polylysine (EPL) as functional excipient...
August 24, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28804018/anti-biofilm-activity-of-a22-s-3-4-dichlorobenzyl-isothiourea-hydrochloride-against-pseudomonas-aeruginosa-influence-on-biofilm-formation-motility-and-bioadhesion
#17
Pauline Cordenonsi Bonez, Grazielle Guidolin Rossi, Jardel Rodrigo Bandeira, Andiara Prates Ramos, Caren Rigon Mizdal, Vanessa Albertina Agertt, Eloísa Salete Segatto Dalla Nora, Márcia Ebling de Souza, Camilla Fillippi Dos Santos Alves, Fallon Siqueira Dos Santos, André Gündel, Rodrigo de Almeida Vaucher, Roberto Christ Vianna Santos, Marli Matiko Anraku de Campos
Bacterial biofilms are involved in various medical infections and for this reason it is of great importance understanding adhesion mechanisms of involved microorganisms is essential to develop new strategies of prevention and control. Different approaches have been used for preventing biofilm related infections in health care settings, such as use of surface coatings agents in medical implants. In this context, is necessary to explore new compounds with anti-biofilm activity. Thus, this study evaluated for the first time the action of A22 against biofilms of Pseudomonas aeruginosa PAO1 strain and multi-resistant clinical isolates on biotic and abiotic surfaces...
October 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28750895/genotoxic-evaluation-of-poly-anhydride-nanoparticles-in-the-gastrointestinal-tract-of-mice
#18
T Iglesias, J M Irache, M Butinar, B Turk, A López de Cerain, A Azqueta
Gantrez(®) AN 119-based NPs have been developed as oral drug carriers due to their strong bioadhesive interaction with components of the gastrointestinal mucosa and to their adaptable surface. The use of mannosamine to coat Gantrez(®) AN 119-based NPs results in a high mucus-permeable carrier, able to reach the gastrointestinal epithelium. Although their efficacy to transport a therapeutic agent has been demonstrated, their safety has not yet been thoroughly studied. They have proved to be non-cytotoxic, non-genotoxic and non-mutagenic in vitro; however, the in vivo toxicity profile has not yet been determined...
July 24, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28732712/structure-performance-relationships-of-temperature-responsive-plga-peg-plga-gels-for-sustained-release-of-bone-morphogenetic-protein-2
#19
Ana Santoveña, Cecilia Monzón, Carmen Alvarez-Lorenzo, Carlos Del Rosario, Araceli Delgado, Carmen Evora, Angel Concheiro, Matias Llabrés, José B Fariña
PLGA (poly(lactic-co-glycolic) acid)-PEG (polyethylene glycol)-PLGA synthesis conditions have an impact on the physicochemical features of the copolymer and its usefulness as biomaterial. This study reports on an analysis of the composition and structural properties of PLGA-PEG-PLGA copolymers applying a variety of analytical techniques. Viscoelastic properties and particularly the temperature-responsive behavior of PLGA-PEG-PLGA showed a marked dependence on copolymer structural features. Physicochemical and biological properties, such as bioadhesion, biocompatibility and cell viability, of the raw copolymers and their gels were also evaluated...
July 19, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28707165/design-preparation-and-evaluation-of-hpmc-based-paa-or-sa-freeze-dried-scaffolds-for-vaginal-delivery-of-fluconazole
#20
Carmen Anatolia Gafitanu, Daniela Filip, Corina Cernatescu, Daniela Rusu, Cristina Gabriela Tuchilus, Doina Macocinschi, Mirela-Fernanda Zaltariov
PURPOSE: Aim of this work was preparation of bioadhesive gel formulations based on Hydroxypropyl methylcellulose (HPMC), Poly(acrylic acid) (PAA) or Sodium alginate (SA) loaded with anise/fluconazole β-cyclodextrin inclusion complexes in 1:2 and 1:3 ratios intended for vaginal applications. METHODS: Freeze-drying method was effectively utilized and superporous morphology was obtained. The superporous morphology of the lyophilized gels, dynamic water vapor sorption measurements, drug release kinetics studies and their antimicrobial activities are presented...
July 13, 2017: Pharmaceutical Research
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