Combinatorial Therapeutic Drug Delivery of Riboflavin and Olopetadine for the Treatment of Keratoconus Affected Corneas of Mice

2019 ◽  
Vol 9 (5) ◽  
pp. 668-672
Author(s):  
Geqiang Yang ◽  
Yushun Xue ◽  
Yanni Zhu ◽  
Ying Qin ◽  
Jing Zhang
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
Methyl Cellulose ◽  
Therapeutic Drug ◽  
The Novel ◽  
Mice Model ◽  
Gelation Temperature ◽  
Gelling Temperature ◽  
Thermoreversible Gel ◽  
Evaluation Parameters

The present study deals with the development and evaluation of novel thermoreversible gel containing Riboflavin and Olopatadine for the treatment of Keratoconus. The novel gel was prepared by using polymers like Poloxamer and hydroxypropyl methyl cellulose (HPMC) using cold method. The formulated system was evaluated for clarity, appearance, pH, gelling temperature, ex vivo diffusion study, Isotonicity, hemolytic study and effect in keratoconus affected mice model. The results showed that formulated gel was found to be clear and transparent having high gelling capacity. The pH was found between 6.5 to 6.9 and gelation temperature between 34 to 37 °C. All formulations were found isotonic and the hemolytic study performed proved the non-hemolytic nature of formulation. Drug content was also within acceptable limit. The F5 formulation was found to be optimized considering all evaluation parameters. F5 formulation showed maximum amount of release (98.5 and 99.6% for Ribo and Olo respectively) within 8 hrs as compare to other formulations. The effect of formulation on keratoconus affected mice showed that matrix can be produced after stimulation of KC cells and the increased thickness can be result of increase number of cells or matrix produced per cell. These results clearly conclude the potential of combinatorial therapeutic drug delivery of riboflavin and olopetadine for the treatment of keratoconus affected corneas of mice.

scholarly journals SCIDOT-18. NANOTHERAPEUTICS FOR NEUROSURGICALLY-APPLIED DRUG DELIVERY

2019 ◽  
Vol 21 (Supplement_6) ◽  
pp. vi275-vi275
Author(s):  
Catherine Vasey ◽  
Vincenzo Taresco ◽  
Stuart Smith ◽  
Cameron Alexander ◽  
Ruman Rahman
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
Drug Formulation ◽  
Local Drug Delivery ◽  
Resection Margins ◽  
Therapeutic Drug ◽  
Tumour Resection ◽  
Combination Drug ◽  
Drug Encapsulation ◽  
Drug Concentrations

Abstract Design and implementation of innovative local drug delivery systems (DDS) may overcome current limitations in GBM treatment, such as the lack of therapeutic drug concentrations reaching residual GBM cells following surgery. Here we describe a novel DDS which utilises a bespoke mechanically engineered spray device, designed for safe surgical use, to deliver a mucoadhesive hydrogel containing chemotherapeutic nanoparticles (NPs) into the tumour resection margins. The overall aim is to spray a NP and polymer solution onto the resection cavity and potentially increase penetration of anti-cancer drugs within the 2 cm reoccurrence zone beyond the infiltrative margin. The mucoadhesive gel of choice, pectin, is currently used in other in vivo applications; however we have repurposed this for the brain. Pectin is biocompatible with GBM and human astrocyte cells in vitro and showed neither toxicity nor inflammation for up to 2 weeks upon orthotopic brain injection. Pectin is biodegradable in artificial CSF and is capable of being sprayed from the engineered device. A panel of polymeric, oil-based and polymer-coated NPs have been developed and optimised to maximise drug encapsulation of etoposide and olaparib as proof-of-concept for combination drug delivery. Etoposide/olaparib was chosen due to cytotoxicity from 5 GBM cell lines, including primary lines isolated from the invasive tumour margin (Mean IC50 of 1.1 µM and 8.3 µM respectively). The optimal NP/drug formulation (based on drug encapsulation, spray capability and bio-adhesiveness) will ultimately be assessed for tolerability and efficacy using orthotopic allograft and xenograft high-grade glioma models, including measurement of penetration of drug/nanoparticle in ex vivo murine and porcine brain using novel hybrid time-of-flight/Orbitrap TM secondary ion mass spectrometer (orbiSIMS) technology.

Transdermal Delivery of Ondansetron HCl from Thermoreversible Gel Containing Nanocomposite

2019 ◽  
Vol 4 (2) ◽  
pp. 137-147 ◽  
Author(s):  
Rabinarayan Parhi ◽  
Surya Santhosh Reddy ◽  
Suryakanta Swain
Keyword(s):  
Drug Release ◽  
Mechanical Strength ◽  
Ex Vivo ◽  
Poloxamer 407 ◽  
Gelation Temperature ◽  
Permeation Study ◽  
Ex Vivo Permeation ◽  
Model Animal ◽  
Ex Vivo Permeation Study ◽  
Thermoreversible Gel

Background: Application of thermoreversible gel can be a solution to the low residence time of the topical dosage forms such as normal gel, ointment and cream on the skin surface. Addition of another polymer and a nanocomposite can improve the poor mechanical strength and fast drug release of poloxamer 407 (POL 407) gel. Therefore, it is essential to add xanthan gum (XG) and graphene oxide (GO, thickness 1-2 nm, lateral dimension 1-5 µm) to POL 407 gel to enhance the mechanical strength and to sustain the drug release from the gel. Methods: Thermal gel of ondansetron hydrochloride (OSH) containing nanocomposite was prepared by adopting cold method. Interaction between drug and polymers was studied using FTIR method, morphological investigation was carried out by optical and scanning electron microscopy method, and rheological study was performed employing rotational rheometer equipped with a cone/plate shear apparatus, gelation temperature by glass bottle method and ex vivo permeation study was performed with cylindrical glass diffusion cell. Skin irritation potential was measured using rat as a model animal. Results: The FTIR spectrum of the selected gel showed that there is shifting of O-H stretching vibration of a hydroxyl group from 3408.72 to 3360.49 cm-1 and appearance of a new band at 1083.01 cm-1. The spectrum of the selected gel also showed the absence of characteristic peaks of GO at 1625.49 cm- 1. This result indicated that there may be an interaction between OSH and GO and hydrogen bonding between XG and POL 407. The gelation temperature was found to be decreased with the increase in GO content from 14.1±1.21°C 13±0.97°C. SEM micrograph demonstrated the uniform dispersion and intercalation of GO sheets in the gel. All the gel formulations showed a pseudo-plastic flow. Ex vivo permeation study (for 24 hr) exhibited highest (6991.425 µg) and lowest (2133.262 µg) amount of drug release, for OG1 and OG5, respectively. This is attributed to an increase in viscosity which led to a decrease in drug permeation across the abdominal skin of rats. The OG1 formulation (without GO) showed the highest flux of 76.66 µg/cm2/h, permeability coefficient (Kp) of 5.111× 10-3 cm/h and enhancement ratio of 3.277 compared to OG5 containing highest amount (9% w/w) of GO. The selected gel was found to be physically stable and there was minimum irritation score. Conclusion: All the above results indicated that thermal gel containing nanocomposite sustained the drug release and can be considered as an alternative to the orally administered tablet of OSH.

Imidazolium-Based Ionic Liquid-Assisted Preparation of Nano-Spheres Loaded with Bio-Active Peptides to Decrease Inflammation in an Osteoarthritis Model: Ex Vivo Evaluations

2021 ◽  
Vol 17 (5) ◽  
pp. 859-872
Author(s):  
Yingzhuo Song ◽  
Tao Zhang ◽  
Huiguang Cheng ◽  
Wei Jiang ◽  
Pu Li ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ex Vivo ◽  
Cartilage Explants ◽  
Therapeutic Drug ◽  
Therapeutic Peptides ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Osteoarthritis is one of the most prevalent chronic diseases. Cartilage inflammation in osteoarthritis results from pain in articular joints. Anti-inflammatory drugs provide relief by hindering the production of pro-inflammatory cytokines and interleukin-6. Targeted delivery of anti-inflammatory drugs is very effective in the treatment of osteoarthritis. This approach reduces the usage of therapeutic drug dosages and unwanted side effects. Here, we fabricated a non-invasive and efficient targeted drug delivery system to reduce persistent inflammation in an osteoarthritis model. Temperature-sensitive hollow dextran/poly(N-isopropyl acrylamide) nanoparticles were synthesized by the destruction of N,N’-bis(acryloyl)cystamine crosslinked cores in imidazolium-based ionic liquids. The copolymerized 2-acrylamido-2-methylpropane sulfonic acid created sulfur functionalities that increase the loading of therapeutic KAFAK peptides. The chemical structure of the polymer nanoparticles was analyzed with UV-Visible, Fourier transform infrared, and X-ray photoelectron spectroscopy. The thermal responsive characteristics of the nanoparticles were determined with dynamic light scattering, scanning electron microscopy, and transmission electron microscopy analyses. Moreover, the synthesized nanoparticles were used as drug carriers to reduce inflammation in an Ex Vivo osteoarthritis model. The KAFAK-loaded hollow dextran/PNIPAM nanoparticles effectively delivered therapeutic peptides in cartilage explants to suppress inflammation. These thermoresponsive nanoparticles could be an effective drug delivery system to deliver anti-inflammatory therapeutic peptides in a highly osteoarthritic environment.

The novel drug delivery to vascular wall using laser driven thermal balloon: basic study ex vivo

2016 ◽  
Author(s):  
Kao Suganuma ◽  
Rie Homma ◽  
Natsumi Shimazaki ◽  
Emiyu Ogawa ◽  
Tsunenori Arai
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
Vascular Wall ◽  
The Novel ◽  
Basic Study ◽  
Novel Drug ◽  
Thermal Balloon

scholarly journals Ethyl Cellulose and Hydroxypropyl Methyl Cellulose Blended Methotrexate-Loaded Transdermal Patches: In Vitro and Ex Vivo

Polymers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 3455
Author(s):  
Muhammad Shahid Latif ◽  
Abul Kalam Azad ◽  
Asif Nawaz ◽  
Sheikh Abdur Rashid ◽  
Md. Habibur Rahman ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Transdermal Patches ◽  
Percent Moisture ◽  
Vitro Release

Transdermal drug delivery systems (TDDSs) have become innovative, fascinating drug delivery methods intended for skin application to achieve systemic effects. TDDSs overcome the drawbacks associated with oral and parenteral routes of drug administration. The current investigation aimed to design, evaluate and optimize methotrexate (MTX)-loaded transdermal-type patches having ethyl cellulose (EC) and hydroxypropyl methyl cellulose (HPMC) at different concentrations for the local management of psoriasis. In vitro release and ex vivo permeation studies were carried out for the formulated patches. Various formulations (F1–F9) were developed using different concentrations of HPMC and EC. The F1 formulation having a 1:1 polymer concentration ratio served as the control formulation. ATR–FTIR analysis was performed to study drug–polymer interactions, and it was found that the drug and polymers were compatible with each other. The formulated patches were further investigated for their physicochemical parameters, in vitro release and ex vivo diffusion characteristics. Different parameters, such as surface pH, physical appearance, thickness, weight uniformity, percent moisture absorption, percent moisture loss, folding endurance, skin irritation, stability and drug content uniformity, were studied. From the hydrophilic mixture, it was observed that viscosity has a direct influence on drug release. Among all formulated patches, the F5 formulation exhibited 82.71% drug release in a sustained-release fashion and followed an anomalous non-Fickian diffusion. The permeation data of the F5 formulation exhibited about a 36.55% cumulative amount of percent drug permeated. The skin showed high retention for the F5 formulation (15.1%). The stability study indicated that all prepared formulations had very good stability for a period of 180 days. Therefore, it was concluded from the present study that methotrexate-loaded transdermal patches with EC and HPMC as polymers at different concentrations suit TDDSs ideally and improve patient compliance for the local management of psoriasis.

Potential Ganciclovir Liposomal Thermoreversible Gel for Ophthalmic Delivery Using Box-Behnken Statistical Design and Efficacy Assessment Study in Rabbit Model

2019 ◽  
Vol 9 (7) ◽  
pp. 950-957
Author(s):  
Yanjuan Sheng ◽  
Yanni Zhu
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Rabbit Model ◽  
Methyl Cellulose ◽  
Temperature Sensitive ◽  
Potential Candidate ◽  
Core System ◽  
Thermoreversible Gel

The present study focuses on development of novel thermoreversible ophthalmic drug delivery system using Ganciclovir as potential candidate for treatment of various ocular infections. The formulation was prepared for thermoreversible gel which incorporates liposomes of Ganciclovir as core system. Thermoreversible gel prolongs delivery of drug with use of combination of polymers like Poloxamer, Hydroxypropyl methyl cellulose. The Poloxamer used here serves as temperature sensitive polymer. Thus prepared system was evaluated for various parameters. Liposomes found to be complies with basic requirement like non-leak ability, high in-vitro drug release with optimum encapsulation efficiency. The results obtained showed that the in situ gel is clear and transparent (prime requirement for ophthalmic product) with high gelling capacity and moderately viscous liquid (1454 cp), highest bioadhesive strength (Dyne/cm2). The ex-vivo study was also done and compared with marketed eye drop formulation. The results showed superiority of in situ gel formulation over eye in sustaining the drug release over prolong period of time. The haemolytic study performed proved the non-haemolytic nature of formulation.

A Review on Fast Dissolving Tablet

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Sagar T. Malsane ◽  
Smita S. Aher ◽  
R. B. Saudagar
Keyword(s):  
Drug Delivery ◽  
Patient Compliance ◽  
Research Area ◽  
Oral Route ◽  
Dosage Forms ◽  
The Novel ◽  
The Past ◽  
Orally Disintegrating Tablets ◽  
Novel Drug ◽  
Experience Difficulty

Oral route is presently the gold standard in the pharmaceutical industry where it is regarded as the safest, most economical and most convenient method of drug delivery resulting in highest patient compliance. Over the past three decades, orally disintegrating tablets (FDTs) have gained considerable attention due to patient compliance. Usually, elderly people experience difficulty in swallowing the conventional dosage forms like tablets, capsules, solutions and suspensions because of tremors of extremities and dysphagia. In some cases such as motion sickness, sudden episodes of allergic attack or coughing, and an unavailability of water, swallowing conventional tablets may be difficult. One such problem can be solved in the novel drug delivery system by formulating “Fast dissolving tablets” (FDTs) which disintegrates or dissolves rapidly without water within few seconds in the mouth due to the action of superdisintegrant or maximizing pore structure in the formulation. The review describes the various formulation aspects, superdisintegrants employed and technologies developed for FDTs, along with various excipients, evaluation tests, marketed formulation and drugs used in this research area.

Self Microemulsifying Nutraceutical and Drug Delivery Systems

2014 ◽  
Vol 7 (3) ◽  
pp. 2520-2528 ◽  
Author(s):  
Vikrant P Wankhade ◽  
Nivedita S Kale ◽  
K.K Tapar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Aqueous Solubility ◽  
Oral Formulation ◽  
Water Soluble ◽  
Drug Dissolution ◽  
The Novel ◽  
Peristaltic Movement

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.

Novel Herbal Topical Patch Containing Curcumin and Arnica montana for the Treatment of Osteoarthritis

2020 ◽  
Vol 16 (1) ◽  
pp. 43-60 ◽  
Author(s):  
Priyanka Kriplani ◽  
Kumar Guarve ◽  
Uttam Singh Baghel
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Analgesic Activity ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Methyl Cellulose ◽  
World Population ◽  
Jojoba Oil ◽  
Arnica Montana ◽  
Transdermal Patches

Background: Osteoarthritis (OA) ranks fifth among all forms of disability affecting 10% of the world population. Current treatments available are associated with multiple side effects and do not slow down the progression of the disease. Moreover, no such effective treatment is available to date in various systems of medicine to treat osteoarthritis. Curcumin and Arnica have shown evident clinical advances in the treatment of osteoarthritis. Objective: The aim of the present study was to design, optimize and characterize novel herbal transdermal patches of curcumin and Arnica montana using factorial design. Methods: A multiple factorial design was employed to investigate the effect of hydroxypropyl methyl cellulose, ethyl cellulose and jojoba oil on elongation and drug release. Transdermal patches were evaluated by FTIR, DSC, FESEM, ex vivo drug permeation, anti osteoarthritic activity and analgesic activity. Results: Independent variables exhibited a significant effect on the physicochemical properties of the prepared formulations. The higher values of drug release and elongation were observed with the higher concentration of hydroxypropyl methylcellulose and jojoba oil. Anti osteoarthritic activity was assessed by complete Freund's adjuvant arthritis model; using rats and analgesic activity by Eddy's hot plate method, using mice. Combination patch exhibited good anti osteoarthritic and analgesic activity as compare to individual drug patches. Conclusion: The design results revealed that the combination patch exhibited good physicochemical, anti osteoarthritic and analgesic activity for the treatment of osteoarthritis in animals. More plants and their combinations should be explored to get reliable, safe and effective formulations that can compete with synthetic drugs.

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