scholarly journals Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug Carriers

Polymers ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 1213 ◽  
Author(s):  
Miguel Gómez-Ballesteros ◽  
Vanessa Andrés-Guerrero ◽  
Francisco Parra ◽  
Jorge Marinich ◽  
Beatriz de-las-Heras ◽  
...  
Keyword(s):  
Intraocular Pressure ◽  
In Vitro Release ◽  
Anterior Segment ◽  
Drug Carriers ◽  
Eye Drops ◽  
Hypotensive Drug ◽  
Ocular Drugs ◽  
Ophthalmic Drug ◽  
Conventional Solution

Topical application of drops containing ocular drugs is the preferred non-invasive route to treat diseases that affect the anterior segment of the eye. However, the formulation of eye drops is a major challenge for pharmacists since the access of drugs to ocular tissues is restricted by several barriers. Acetazolamide (ACZ) is a carbonic anhydrase inhibitor used orally for the treatment of ocular hypertension in glaucoma. However, large ACZ doses are needed which results in systemic side effects. Recently, we synthesized copolymers based on 2-hydroxyethyl methacrylate (HEMA) and a functionalized three-arm poloxamer star (Bayfit-MA). The new material (HEMA/Bayfit-MA) was engineered to be transformed into nanoparticles without the use of surfactants, which represents a significant step forward in developing new ophthalmic drug delivery platforms. Acetazolamide-loaded nanocarriers (ACZ-NPs) were prepared via dialysis (224 ± 19 nm, −17.2 ± 0.4 mV). The in vitro release rate of ACZ was constant over 24 h (cumulative delivery of ACZ: 83.3 ± 8.4%). Following standard specifications, ACZ-NPs were not cytotoxic in vitro in cornea, conjunctiva, and macrophages. In normotensive rabbits, ACZ-NPs generated a significant intraocular pressure reduction compared to a conventional solution of ACZ (16.4% versus 9.6%) with the same dose of the hypotensive drug (20 µg). In comparison to previously reported studies, this formulation reduced intraocular pressure with a lower dose of ACZ. In summary, HEMA:Bayfit-MA nanoparticles may be a promising system for ocular topical treatments, showing an enhanced ocular bioavailability of ACZ after a single instillation on the ocular surface.

scholarly journals Nanotechnology for Topical Drug Delivery to the Anterior Segment of the Eye

2021 ◽  
Vol 22 (22) ◽  
pp. 12368
Author(s):  
Alexander Vaneev ◽  
Victoria Tikhomirova ◽  
Natalia Chesnokova ◽  
Ekaterina Popova ◽  
Olga Beznos ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Anterior Segment ◽  
Drug Carriers ◽  
Ocular Tissue ◽  
Eye Drops ◽  
Topical Drug Delivery ◽  
Natural Polymers ◽  
Drug Bioavailability ◽  
Sustained Drug Release

Topical drug delivery is one of the most challenging aspects of eye therapy. Eye drops are the most prevalent drug form, especially for widely distributed anterior segment eye diseases (cataracts, glaucoma, dry eye syndrome, inflammatory diseases, etc.), because they are convenient and easy to apply by patients. However, conventional drug formulations are usually characterized by short retention time in the tear film, insufficient contact with epithelium, fast elimination, and difficulties in overcoming ocular tissue barriers. Not more than 5% of the total drug dose administered in eye drops reaches the interior ocular tissues. To overcome the ocular drug delivery barriers and improve drug bioavailability, various conventional and novel drug delivery systems have been developed. Among these, nanosize carriers are the most attractive. The review is focused on the different drug carriers, such as synthetic and natural polymers, as well as inorganic carriers, with special attention to nanoparticles and nanomicelles. Studies in vitro and in vivo have demonstrated that new formulations could help to improve the bioavailability of the drugs, provide sustained drug release, enhance and prolong their therapeutic action. Promising results were obtained with drug-loaded nanoparticles included in in situ gel.

scholarly journals Ophthalmic Drug Dosage Forms: Characterisation and Research Methods

2014 ◽  
Vol 2014 ◽  
pp. 1-14 ◽  
Author(s):  
Przemysław Baranowski ◽  
Bożena Karolewicz ◽  
Maciej Gajda ◽  
Janusz Pluta
Keyword(s):  
Defense Mechanisms ◽  
Drug Application ◽  
Drug Dosage ◽  
Eye Drops ◽  
Eye Tissues ◽  
Ophthalmic Drug ◽  
Application Frequency

This paper describes hitherto developed drug forms for topical ocular administration, that is, eye drops, ointments,in situgels, inserts, multicompartment drug delivery systems, and ophthalmic drug forms with bioadhesive properties. Heretofore, many studies have demonstrated that new and more complex ophthalmic drug forms exhibit advantage over traditional ones and are able to increase the bioavailability of the active substance by, among others, reducing the susceptibility of drug forms to defense mechanisms of the human eye, extending contact time of drug with the cornea, increasing the penetration through the complex anatomical structure of the eye, and providing controlled release of drugs into the eye tissues, which allows reducing the drug application frequency. The rest of the paper describes recommendedin vitroandin vivostudies to be performed for various ophthalmic drugs forms in order to assess whether the form is acceptable from the perspective of desired properties and patient’s compliance.

Formulation and Evaluation of Ophthalmic Antibacterial Gels and Comparison of Different Polymers Using Factorial Design

2020 ◽  
Vol 3 (3) ◽  
pp. 01-07
Author(s):  
Alka Ahuja
Keyword(s):  
Factorial Design ◽  
Drug Delivery Systems ◽  
In Vitro Release ◽  
Hydroxypropyl Cellulose ◽  
Eye Drops ◽  
Eye Infections ◽  
Preparation And Evaluation ◽  
Vitro Release ◽  
Ophthalmic Solutions

Different formulations for the treatment of eye infections are usually administered in the form of conventional ocular drug delivery systems which are topical eye drops or ointments (1). Typically ophthalmic bioavailabilities of only 1–10% are achieved due to the short precorneal residence time of ophthalmic solutions. (2) The preparation and evaluation of gel containing antibiotic azithromycin combined with different polymers like Carbopol, sodium alginate and Hydroxypropyl cellulose (HPC) was done and assessed to find out which polymer could best be used in preparing ophthalmic gels for this antibiotic using factorial design. Since the efficacy of these gels is dependent on factors like viscosity and pH, the polymers in these gels were also examined for different parameters such as pH, in vitro release, permeation and microbiological evaluation.

scholarly journals A Facile Route to Fabricate CS/GO Composite Film for the Application of Therapeutic Contact Lenses

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Pin Chen ◽  
Xin Wang ◽  
Jingyang Kong ◽  
Xiaohong Hu
Keyword(s):  
Composite Film ◽  
Contact Lenses ◽  
Umbilical Vein ◽  
Drug Carriers ◽  
Diffusion Method ◽  
Swelling Ratio ◽  
Significant Difference ◽  
Ophthalmic Drug ◽  
Model Drug

Traditional contact lenses bring convenience for ophthalmic drug delivery. However, either as contact lenses or as drug carriers, traditional materials have still some drawbacks in the field. Therefore, a transparent film was designed and investigated for the application of therapeutic contact lenses. Chitosan (CS)/graphene oxide (GO) composite film and CS film were fabricated with acceptable transparent and tensile properties by simple casting flow method. Although swelling ratio of CS/GO composite film was higher than that of CS film with significant difference, both formed films had suitable swelling ratio for contact lens application. Both CS/GO composite film and CS film exhibited typical CS infrared characteristic peaks. CS/GO composite film had significant greater breaking strength than CS film, but its elongation at break was a little lower than CS film. Either CS/GO composite film or CS film exhibited good hydrophilic property with a contact angle of around 20 degree. Ofloxacin as a model drug was loaded into films by adsorption diffusion method. Loaded drug amount in CS/GO composite film was a little larger than that in CS film, but without significant difference. The drug release behaviors from CS/GO composite film or CS film were investigated and revealed that the loaded drug could be controlled to release in the first hour. Two kinds of cells were used to evaluate the biocompatibility of films by in vitro method. It was found that both CS/GO composite film and CS film could support human umbilical vein endothelial cell (HUVEC) growth. But for human epidermal fibroblasts (HSF) cells, CS/GO composite film could promote HSF cells growth and proliferation much better than CS film.

scholarly journals Synthesis and Characterization of pH-Responsive PEG-Poly(β-Amino Ester) Block Copolymer Micelles as Drug Carriers to Eliminate Cancer Stem Cells

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 111 ◽  
Author(s):  
Weinan Li ◽  
Jialin Sun ◽  
Xiaoyu Zhang ◽  
Li Jia ◽  
Mingxi Qiao ◽  
...  
Keyword(s):  
Stem Cells ◽  
Cancer Stem Cells ◽  
Drug Loading ◽  
In Vitro Release ◽  
Drug Carriers ◽  
Breast Cancer Cell Lines ◽  
Fluorescence Signal ◽  
Amino Ester ◽  
Ph Responsive

PEG-poly(β-amino ester) (PEG-PBAE), which is an effective pH-responsive copolymer, was mainly synthesized by Michael step polymerization. Thioridazine (Thz), which was reported to selectively eliminate cancer stem cells (CSCs), was loaded into PEG-PBAE micelles (PPM) prepared by self-assembly at low concentrations. The critical micelle concentrations (CMC) of PPM in water were 2.49 μg/mL. The pH-responsive PBAE segment was soluble due to protonated tertiary amine groups when the pH decreased below pH 6.8, but it was insoluble at pH 7.4. The Thz-loaded PEG-PBAE micelle (Thz/PPM) exhibited a spherical shape, and the drug loading was 15.5%. In vitro release of Thz/PPM showed that this pH-sensitivity triggered the rapid release of encapsulated Thz in a weakly acidic environment. The in vitro cytotoxicity and cellular uptake of various formulations at pH 7.4 and 5.5 were evaluated on the mammospheres (MS), which were sorted by MCF-7 human breast cancer cell lines and identified to be a CD44+/CD24− phenotype. The results of the cytotoxicity assay showed that blank micelles were nontoxic and Thz/PPM exhibited a similar anti-CSC effect on MS compared to Thz solution. Stronger fluorescence signal of Coumarin-6 (C6) was observed in MS treated by C6-loaded PPM (C6/PPM) at pH 5.5. The tumor inhibition rate and tumor weight of the free DOX and Thz/PPM groups were significantly different from those of the other groups, which free DOX and Thz/PPM effectively suppressed breast tumor growth in vivo. The above experimental results showed that Thz/PPM is an ideal and effective pH-responsive drug delivery carrier to a targeted therapy of CSCs.

scholarly journals Novel Contact Lenses Embedded with Drug-Loaded Zwitterionic Nanogels for Extended Ophthalmic Drug Delivery

Nanomaterials ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 2328
Author(s):  
Zhao Wang ◽  
Xinhua Li ◽  
Xiaojuan Zhang ◽  
Ruilong Sheng ◽  
Qing Lin ◽  
...  
Keyword(s):  
Drug Release ◽  
Contact Lenses ◽  
Eye Drops ◽  
Water Contact ◽  
In Vitro Drug Release ◽  
Molding Method ◽  
Ophthalmic Drug ◽  
One Step

Therapeutic ophthalmic contact lenses with prolonged drug release and improved bioavailability have been developed to circumvent tedious eye drop instillation. In this work, zwitterionic nanogels based on poly(sulfobetaine methacrylate) (PSBMA) were easily fabricated by one-step reflux-precipitation polymerization, with the advantages of being surfactant-free and morphology controlled. Then, the ophthalmic drug levofloxacin (LEV) was encapsulated into the nanogels. A set of contact lenses with varied nanogel-loading content was fabricated by the cast molding method, with the drug-loaded nanogels dispersed in pre-monomer solutions composed of 2-hydroxyethyl methacrylate (HEMA) and N-vinyl-2-pyrrolidone (NVP). The structure, surface morphology, water contact angle (WCA), equilibrium water content (EWC), transmittance, and mechanical properties of the contact lenses were subsequently investigated, and in vitro drug release and biocompatibility were further evaluated. As a result, the optimized contact lens with nanogel-loading content of 8 wt% could sustainably deliver LEV for ten days, with critical lens properties within the range of recommended values for commercial contact lenses. Moreover, cell viability assays revealed that the prepared contact lenses were cytocompatible, suggesting their significant potential as an alternative to traditional eye drops or ointment formulations for long-term oculopathy treatment.

scholarly journals Preparation, characterization, and in vitro evaluation of amphiphilic peptide P12 and P12-DOX nanomicelles as antitumor drug carriers

2020 ◽  
Vol 10 ◽  
pp. 184798042091151 ◽  
Author(s):  
Ping Song ◽  
Wuchen Du ◽  
Wanzhen Li ◽  
Longbao Zhu ◽  
Weiwei Zhang ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Phase ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Drug Carriers ◽  
Average Particle ◽  
Polymer Micelles ◽  
Amphiphilic Peptide

Polymerized polypeptide nanomicelles have attracted much attention as novel drug carriers because of their good biocompatibility and degradability. To prepare doxorubicin (DOX)-loaded nanomicelles, an amphiphilic peptide, FFHFFH-KKGRGD (P12), was synthesized by solid-phase synthesis, and the physicochemical and drug-release properties, as well as the cytotoxicity of the nanomicelles, were evaluated in vitro. The P12-DOX polymer micelles were prepared by dialysis. The morphology and particle size were characterized by transmission electron microscopy and dynamic light scattering. The critical micelle concentration (CMC) of the polymer was determined by the probe method, and the drug-release characteristics of the micelles were studied by dynamic dialysis. The cytotoxicity and uptake of the P12-DOX micelles were evaluated against mouse breast cancer cells (4T1) and human umbilical vein endothelial cells. The peptide polymer micelles containing DOX were uniformly sized and had a spherical core–shell structure with an average particle size of 128.6 nm. The CMC of the polymer was low (0.0357 mg/mL). The in vitro release of DOX from the micelles is slow and is consistent with first-order kinetics. The copolymer micelles of the P12 polypeptide and DOX can be used as nanoscale spherical carriers of hydrophobic drugs and have broad applicability.

scholarly journals The Efficient Apoptotic Induction of Paclitaxel-Loaded Poly(N-vinylpyrrolidone)-block-poly(ε-caprolactone) Nanoparticles in the In Vitro Study of Lung Cancer Cell Lines

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Donghui Zheng ◽  
Huiping Ye ◽  
Can Luo ◽  
Huae Xu ◽  
Ling Meng
Keyword(s):  
Lung Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
In Vitro Release ◽  
Drug Carriers ◽  
Cancer Cell Lines ◽  
Severe Adverse Effect ◽  
Lung Cancer Cell ◽  
Nanodrug Delivery

Paclitaxel (Ptx) has been established as one of the most important components of first line chemotherapy regimen in the treatment of lung cancer. However, the poor solubility of Ptx makes it employ Cremophor as a solvent, which greatly limits its application due to the severe adverse effect. Encapsulation of Ptx into nanoparticles substantially increases the solubility of Ptx, therefore eradicating the necessity of Cremophor involvement. Here we report on a simple way of preparing Ptx-loaded nanoparticles formed by amphiphilic poly(N-vinylpyrrolidone)-block-poly(ε-caprolactone) (PVP-b-PCL) copolymers. Ptx was incorporated into PVP-b-PCL nanoparticles with a high loading efficiency. In vitro release study shows that Ptx was released from the nanoparticles in a sustained manner. The following experiments including cell staining and cytotoxicity tests indicated that Ptx-NPs led to enhanced induction of apoptosis in non-small-cell lung cancer cell lines NCI-1975 and A549, which is achieved by regulating the expression of apoptosis related proteins. Therefore, data from this study offers an effective way of improving the anticancer efficiency of Ptx by a nanodrug delivery system with amphiphilic PVP-b-PCL as drug carriers.

scholarly journals OPTIMIZATION AND CHARACTERIZATION OF ION ACTIVATED OCULAR IN-SITU GEL FORMULATION FOR BACTERIAL CONJUNCTIVITIS

2020 ◽  
pp. 182-191
Author(s):  
ANKITA KAPOOR ◽  
G. D. GUPTA
Keyword(s):  
Research Work ◽  
In Vitro Release ◽  
Gellan Gum ◽  
Log P ◽  
Eye Drops ◽  
Bacterial Conjunctivitis ◽  
In Situ Gel ◽  
Vitro Release

Objective: The present research work aims at describing the formulation, optimization and evaluation of ion activated ocular in-situ gel of gatifloxacin for treatment of bacterial conjunctivitis so as to overcome patient inconvenience, precorneal drug elimination, variation in efficacy, vision blurring and frequent instillation associated with conventional eye drops and ointments. Methods: In-situ gel was prepared using gellan gum as an ion activated phase transition polymer and HPMC K100M as release retardant. Gatifloxacin was characterized by spectrophotometry. Crystalline state of the drug was determined using X Ray Diffraction study. The developed formulation exhibited instantaneous gel formation in simulated lacrimal fluid (pH 7.4), which was further evaluated for its rheology, irritancy parameters, in vitro release, trans-corneal permeation and antimicrobial activity. Results: Gatifloxacin exhibited λmax 286 nm obeying Beer Lambert’s law and pH-dependent solubility at a pH range of 2 to 4. 0.6% gellan gum and 0.4% HPMC K100M were optimized in the formulation which exhibited a viscosity of 55 cps in sol form and 325 cps in gel form with pseudoplastic behavior and prolonged in vitro release. Permeation of formulation was 75.8% in 7 h with log P of drug 0.59. Developed isotonic and non-irritant formulation had a lower apparent permeability coefficient of 8.15 x 10-5 cm/sec as compared to marketed formulation. Conclusion: A Formulation can be viewed as an efficacious medicine by virtue of its higher zone of inhibition, ability to enhance precorneal residence time and consequently ocular bioavailability with lesser frequency of administration attributed to slow and prolonged diffusion of the drug from the polymeric solutions.

scholarly journals Solulan C24- and Bile Salts-Modified Niosomes for New Ciprofloxacin Mannich Base for Combatting Pseudomonas-Infected Corneal Ulcer in Rabbits

2021 ◽  
Vol 15 (1) ◽  
pp. 44
Author(s):  
Soad A. Mohamed ◽  
Mohamed A. Abdelgawad ◽  
Rania Alaaeldin ◽  
Zeinab Fathalla ◽  
Hossam Moharram ◽  
...  
Keyword(s):  
Corneal Ulcer ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sodium Cholate ◽  
Resistance Rate ◽  
Eye Drops ◽  
Global Health Issue ◽  
And Control

Keratitis is a global health issue that claims the eye sight of millions of people every year. Dry eye, contact lens wearing and refractive surgeries are among the most common causes. The resistance rate among fluoroquinolone antibiotics is >30%. This study aims at formulating a newly synthesized ciprofloxacin derivative (2b) niosomes and Solulan C24-, sodium cholate- and deoxycholate-modified niosomes. The prepared niosomal dispersions were characterized macroscopically and microscopically (SEM) and by percentage entrapment efficiency, in vitro release and drug release kinetics. While the inclusion of Solulan C24 produced something discoidal-shaped with a larger diameter, both cholate and deoxycholate were unsuccessful in forming niosomes dispersions. Conventional niosomes and discomes (Solulan C24-modified niosomes) were selected for further investigation. A corneal ulcer model inoculated with colonies of Pseudomonas aeruginosa in rabbits was developed to evaluate the effectiveness of keratitis treatment of the 2b-loaded niosomes and 2b-loaded discomes compared with Ciprocin® (ciprofloxacin) eye drops and control 2b suspension. The histological documentation and assessment of gene expression of the inflammatory markers (IL-6, IL1B, TNFα and NF-κB) indicated that both 2b niosomes and discomes were superior treatments and can be formulated at physiological pH 7.4 compatible with the ocular surface, compared to both 2b suspension and Ciprocin® eye drops.

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