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 ◽  
...  

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.

2020 ◽  
pp. bjophthalmol-2020-315911
Author(s):  
Chee Wai Wong ◽  
Josbert M Metselaar ◽  
Gert Storm ◽  
Tina T Wong

Ocular anterior segment inflammation is a medical problem that is seen in cases of cataract surgery and non-infectious anterior uveitis. Inadequately treated anterior segment inflammation can lead to sight-threatening conditions such as corneal oedema, glaucoma and cystoid macular oedema. The mainstay of treatment for anterior segment inflammation is topical steroid eye-drops. However, several drawbacks limit the critical value of this treatment, including low bioavailability, poor patient compliance, relatively difficult administration manner and risk of blurring of vision and ocular irritation. A drug delivery system (DDS) that can provide increased bioavailability and sustained delivery while being specifically targeted towards inflamed ocular tissue can potentially replace daily eye-drops as the gold standard for management of anterior segment inflammation. The various DDS for anti-inflammatory drugs for the treatment of anterior segment inflammation are listed and summarised in this review, with a focus on commercially available products and those in clinical trials. Dextenza, INVELTYS, Dexycu and Bromsite are examples of DDS that have enjoyed success in clinical trials leading to FDA approval. Nanoparticles and ocular iontophoresis form the next wave of DDS that have the potential to replace topical steroids eye-drops as the treatment of choice for anterior segment inflammation. With the current relentless pace of ophthalmic drug delivery research, the pursuit of a new standard of treatment that eliminates the problems of low bioavailability and patient compliance may soon be realised.


Polymers ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 1213 ◽  
Author(s):  
Miguel Gómez-Ballesteros ◽  
Vanessa Andrés-Guerrero ◽  
Francisco Parra ◽  
Jorge Marinich ◽  
Beatriz de-las-Heras ◽  
...  

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.


2018 ◽  
Vol 18 (2) ◽  
pp. 302-311
Author(s):  
Shulin Dai ◽  
Yucheng Feng ◽  
Shuyi Li ◽  
Yuxiao Chen ◽  
Meiqing Liu ◽  
...  

Background: Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between the equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release. </P><P> Aims/Methods: In this paper, stereocomplexed micelles gama-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(gama-glutamic acid)-graft-PLLA gama-PGA-g-PLA) and poly(gamaglutamic acid)-graft-PDLA gama-PGA-g-PLA). These stereocomplexed micelles exhibited a lower CMC than the corresponding enantiomeric micelles. Result: Furthermore, they showed higher drug loading content and drug loading efficiency in addition to more sustained drug release profile in vitro. In vivo imaging confirmed that the DiR-encapsulated stereocomplexed gama-PGA-g-PLA micelles can deliver anti-cancer drug to tumors with enhanced tissue penetration. Overall, gama-PGA-g-PLA micelles exhibited greater anti-cancer effects as compared with the free drug and the stereocomplexation may be a promising strategy for fabrication of anti-cancer drug carriers with significantly enhanced efficacy.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 608
Author(s):  
Csilla Bartos ◽  
Patrícia Varga ◽  
Piroska Szabó-Révész ◽  
Rita Ambrus

The absorption of non-steroidal anti-inflammatory drugs (NSAIDs) through the nasal epithelium offers an innovative opportunity in the field of pain therapy. Thanks to the bonding of chitosan to the nasal mucosa and its permeability-enhancing effect, it is an excellent choice to formulate microspheres for the increase of drug bioavailability. The aim of our work includes the preparation of spray-dried cross-linked and non-cross-linked chitosan-based drug delivery systems for intranasal application, the optimization of spray-drying process parameters (inlet air temperature, pump rate), and the composition of samples. Cross-linked products were prepared by using different amounts of sodium tripolyphosphate. On top of these, the micrometric properties, the structural characteristics, the in vitro drug release, and the in vitro permeability of the products were studied. Spray-drying resulted in micronized chitosan particles (2–4 μm) regardless of the process parameters. The meloxicam (MEL)-containing microspheres showed nearly spherical habit, while MEL was present in a molecularly dispersed state. The highest dissolved (>90%) and permeated (~45 µg/cm2) MEL amount was detected from the non-cross-linked sample. Our results indicate that spray-dried MEL-containing chitosan microparticles may be recommended for the development of a novel drug delivery system to decrease acute pain or enhance analgesia by intranasal application.


2017 ◽  
Vol 2017 ◽  
pp. 1-16 ◽  
Author(s):  
Lígia N. M. Ribeiro ◽  
Ana C. S. Alcântara ◽  
Gustavo H. Rodrigues da Silva ◽  
Michelle Franz-Montan ◽  
Silvia V. G. Nista ◽  
...  

The use of biomaterials composed of organic pristine components has been successfully described in several purposes, such as tissue engineering and drug delivery. Drug delivery systems (DDS) have shown several advantages over traditional drug therapy, such as greater therapeutic efficacy, prolonged delivery profile, and reduced drug toxicity, as evidenced by in vitro and in vivo studies as well as clinical trials. Despite that, there is no perfect delivery carrier, and issues such as undesirable viscosity and physicochemical stability or inability to efficiently encapsulate hydrophilic/hydrophobic molecules still persist, limiting DDS applications. To overcome that, biohybrid systems, originating from the synergistic assembly of polymers and other organic materials such as proteins and lipids, have recently been described, yielding molecularly planned biohybrid systems that are able to optimize structures to easily interact with the targets. This work revised the biohybrid DDS clarifying their advantages, limitations, and future perspectives in an attempt to contribute to further research of innovative and safe biohybrid polymer-based system as biomaterials for the sustained release of active molecules.


2011 ◽  
Vol 149 (2) ◽  
pp. 159-167 ◽  
Author(s):  
Priya Batheja ◽  
Larisa Sheihet ◽  
Joachim Kohn ◽  
Adam J. Singer ◽  
Bozena Michniak-Kohn

Author(s):  
Anupam K Sachan ◽  
Saurabh Singh ◽  
Kiran Kumari ◽  
Pratibha Devi

Microspheres carrier system made from natural or synthetic polymers used in sustained release drug delivery system. The present study involves formulation and evaluation of floating microspheres of Curcumin for improving the drug bioavailability by prolongation gastric residence time. Curcumin, natural hypoglycemic agent is a lipophilic drug, absorbed poorly from the stomach, quickly eliminated and having short half-life so suitable to formulate floating drug delivery system for sustained release. Floating microspheres of curcumin were formulated by solvent evaporation technique using ethanol and dichloromethane (1:1) as organic solvent and incorporating various synthetic polymers as coating polymer, sustain release polymers and floating agent. The final formulation were evaluated various parameters such as compatibility studies, micrometric properties, In-vitro drug release and % buoyancy. FTIR studies showed that there were no interaction between drug and excipients. The surface morphology studies by SEM confirmed their spherical and smooth surface. The mean particles size were found to be 416-618µm, practical yield of microspheres was in the range of 60.21±0.052% - 80.87±0.043%, drug entrapment efficiency 47.4±0.065% - 77.9±0.036% and % buoyancy 62,24±0.161% - 88.63±0.413%. Result show that entraptmency increased as polymer (Eudragit RS100) conc. Increased. The drug release after 12 hrs. was 72.13% - 87.13% and it decrease as a polymer (HPMC, EC) concentration was decrease.


Author(s):  
SHUBHAM MUKHERJEE ◽  
SUTAPA BISWAS MAJEE ◽  
GOPA ROY BISWAS

Objective: Hydrogels with scope for utilization in numerous fields possess limited applications due to problems in incorporating wide range of drugs and crossing the lipophilic barrier of the skin. Attempts to overcome these problems by developing organogel hold drawbacks. Challenges posed by drug lipophilicity or skin permeation can be solved by developing bigel formed via combination of lipophilic and hydrophilic gel phases in a definite proportion. The objective of the present study is to formulate and characterize matrix type bigel of soybean oil and HPMCK4M for topical drug delivery. Methods: Four batches of bigels were developed with two organogel formulations of soybean oil containing 20 and 22% w/v Span 60. Both organogels and bigels were examined for compatibility by FTIR spectroscopy, hemocompatibility and characterized for physical appearance, pH, rheological behavior and in vitro drug release pattern. Results: FTIR study confirmed compatibility between paracetamol and components of organogel or bigel. The oily feel of organogels disappeared with bigels which possessed a creamy and smooth texture. Pseudoplastic behaviour was confirmed by Ostwald-de wale power-law model in both organogels and bigels. Improved drug release was observed in bigel (BG1) formulation containing 3%w/v HPMCK4M and soybean oil based organogel with 20% w/v Span 60 as compared to the corresponding organogel (OG1). Organogels were foundto follow either zero-order kinetics (OG1) or Korsmeyer-Peppasmodel (OG2) while the formation of matrix was exhibited in bigels with drug diffusion predominantly of non-Fickian type. Conclusion: Therefore, bigels of soybean oil based organogel with HPMCK4M hydrogel formed gel matrix demonstrating improved drug release for topical application compared to organogel.


2012 ◽  
Vol 1 (9) ◽  
pp. 243-249 ◽  
Author(s):  
Sudheshnababu Sukhavasi ◽  
V. Sai Kishore

Fast dissolving/disintegrating tablets have received ever-increasing demand during the last decade, and the field has became a rapidly growing area in the pharmaceutical area. Particularly the fast dissolving drug delivery systems formulated with natural polymers have more demand because natural materials like gums and mucilages have been extensively used in the field of drug delivery for their easy availability, ease administration, non toxicity, non irritant nature etc. The main aim of the present study was to formulate the fast dissolving tablets of amlodipine besylate tablets using Fenugreek seed mucilage and Ocimum basilicum gum as a natural superdisintegrating agents to achieve quick onset of action, is to increase the water uptake with in shortest wetting time and there by decrease the disintegration time of the tablets by simple and cost effective direct compression technique. Pre-compression parameters like angle of repose and post-compression parameters like wetting time, water absorption ratio, in-vitro disintegration and in-vitro dispersion time were studied. The hardness, friability and drug content of all the formulations were found to be within the limits. The best formulations FFGK5 & FOB5 have shown good disintegration time, hardness and friability. The best formulations were also found to be stable. Optimized formulation was subjected to stability studies as per ICH guidelines and it insignificant change in hardness, disintegration time and in vitro drug release.DOI: http://dx.doi.org/10.3329/icpj.v1i9.11614 International Current Pharmaceutical Journal 2012, 1(9): 243-249 


2019 ◽  
Vol 25 (11) ◽  
pp. 1172-1186 ◽  
Author(s):  
Dilshad Qureshi ◽  
Suraj Kumar Nayak ◽  
Samarendra Maji ◽  
Doman Kim ◽  
Indranil Banerjee ◽  
...  

Background: With the advancement in the field of medical science, the idea of sustained release of the therapeutic agents in the patient’s body has remained a major thrust for developing advanced drug delivery systems (DDSs). The critical requirement for fabricating these DDSs is to facilitate the delivery of their cargos in a spatio-temporal and pharmacokinetically-controlled manner. Albeit the synthetic polymer-based DDSs normally address the above-mentioned conditions, their potential cytotoxicity and high cost have ultimately constrained their success. Consequently, the utilization of natural polymers for the fabrication of tunable DDSs owing to their biocompatible, biodegradable, and non-toxic nature can be regarded as a significant stride in the field of drug delivery. Marine environment serves as an untapped resource of varied range of materials such as polysaccharides, which can easily be utilized for developing various DDSs. Methods: Carrageenans are the sulfated polysaccharides that are extracted from the cell wall of red seaweeds. They exhibit an assimilation of various biological activities such as anti-thrombotic, anti-viral, anticancer, and immunomodulatory properties. The main aim of the presented review is threefold. The first one is to describe the unique physicochemical properties and structural composition of different types of carrageenans. The second is to illustrate the preparation methods of the different carrageenan-based macro- and micro-dimensional DDSs like hydrogels, microparticles, and microspheres respectively. Fabrication techniques of some advanced DDSs such as floating hydrogels, aerogels, and 3-D printed hydrogels have also been discussed in this review. Next, considerable attention has been paid to list down the recent applications of carrageenan-based polymeric architectures in the field of drug delivery. Results: Presence of structural variations among the different carrageenan types helps in regulating their temperature and ion-dependent sol-to-gel transition behavior. The constraint of low mechanical strength of reversible gels can be easily eradicated using chemical crosslinking techniques. Carrageenan based-microdimesional DDSs (e.g. microspheres, microparticles) can be utilized for easy and controlled drug administration. Moreover, carrageenans can be fabricated as 3-D printed hydrogels, floating hydrogels, and aerogels for controlled drug delivery applications. Conclusion: In order to address the problems associated with many of the available DDSs, carrageenans are establishing their worth recently as potential drug carriers owing to their varied range of properties. Different architectures of carrageenans are currently being explored as advanced DDSs. In the near future, translation of carrageenan-based advanced DDSs in the clinical applications seems inevitable.


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