scholarly journals Preparation and Evaluation of Eudragit® L100 Nanoparticles LoadedImpregnated with KT Tromethamine Loaded PVA -HEC Insertions forOphthalmic Drug Delivery

2019 ◽  
Vol 9 (4) ◽  
pp. 593-600
Author(s):  
Ghobad Mohammadi ◽  
Shahla Mirzaeei ◽  
Shiva Taghe ◽  
Pardis Mohammadi

Purpose: The purpose of the present study was to improve the ocular delivery for ketorolactromethamine (KT) used to treat inflammation of the eye.Methods: Eudragit nanoparticles loaded with KT were prepared and incorporated in polyvinylalcohol (PVA) and hydroxyethyl cellulose (HEC) films. Nanoparticles were characterized byFourier transform-infrared (FT-IR), scanning electron microscopy (SEM). Physicochemicalproperties and encapsulation effciency were investigated for nanoparticles. Also, the insertswere evaluated for their physiochemical parameters like percentage moisture absorption,percentage moisture loss, thickness and folding endurance.Results: Mean particle size and zeta potential were in range of 153.8-217 nm and (-10.8) -(-40.7) mV, respectively. The results show that the use of a surfactant has not led to any majorchange on drug loading. The loading increases with the amount of polymer. The insert had athickness varying from 0.072 ± 0.0098 to 0.0865 ± 0.0035 mm. The thicknesses of the insertsand the folding endurance increased with the total polymer concentration. The physicochemicalproperties showed that the Eudragit® L-100 nanoparticles loaded PVA-HEC films could be aneffective carrier for KT.Conclusion: For the first time, inserts of Eudragit nanoparticles were successfully prepared forophthalmic drug delivery system to prevent frequent drug administration and enhance patientcompliance.<br />

2021 ◽  
Vol 22 (19) ◽  
pp. 10755
Author(s):  
Chiara Tramontano ◽  
Bruno Miranda ◽  
Giovanna Chianese ◽  
Luca De Stefano ◽  
Carlo Forestiere ◽  
...  

Inorganic diatomite nanoparticles (DNPs) have gained increasing interest as drug delivery systems due to their porous structure, long half-life, thermal and chemical stability. Gold nanoparticles (AuNPs) provide DNPs with intriguing optical features that can be engineered and optimized for sensing and drug delivery applications. In this work, we combine DNPs with gelatin stabilized AuNPs for the development of an optical platform for Galunisertib delivery. To improve the DNP loading capacity, the hybrid platform is capped with gelatin shells of increasing thicknesses. Here, for the first time, full optical modeling of the hybrid system is proposed to monitor both the gelatin generation, degradation, and consequent Galunisertib release by simple spectroscopic measurements. Indeed, the shell thickness is optically estimated as a function of the polymer concentration by exploiting the localized surface plasmon resonance shifts of AuNPs. We simultaneously prove the enhancement of the drug loading capacity of DNPs and that the theoretical modeling represents an efficient predictive tool to design polymer-coated nanocarriers.


Author(s):  
CLINTON JOSE ◽  
SNEH PRIYA ◽  
DIVYA JYOTHI ◽  
HIMANSHU JOSHI ◽  
CYNTHIA LIZZIE LOBO ◽  
...  

Objective: The objective of the present investigation was to design and characterize a mucoadhesive buccal patch of Nebivolol hydrochloride in order to administer a small dose of a drug to treat hypertension effectively and thereby avoiding disadvantages such as patient noncompliance and low bioavailability. Methods: The buccal patches were prepared by solvent casting method. The polymers used to formulate patches were HPMC K 15 M, PVP K 30, and propylene glycol was used as plasticizer and ethanol as the solvent. The drug-polymer compatibility studied was conducted by FTIR. Results: All the developed Patches had good transparency and stability. All formulated patches showed pH in the range of 6.49 to 7.22, and drug content was more than 90%. The folding endurance value showed that the patches are flexible and non-brittle. The in vitro residence time was found to more than 30 min. Thickness, % moisture absorption, and % moisture loss values were in a normal range. The drug release study was conducted for 8 h, and it was found drug release was decreased with the increase in polymer concentration. The in vitro release profiles of the drug from all the formulations appeared to follow Korsmeyer Peppa's exponential model, and release exponent (n) was found to be more than 0.45 so that the release can be characterized by Non–Fickian (anomalous) diffusion. Conclusion: From the results, it was concluded that drug released from formulated buccal patches follows sustained release pattern, Hence can be used for the treatment of the hypertensive patient.


2021 ◽  
Vol 18 (24) ◽  
pp. 1403
Author(s):  
Jamal Moideen Muthu Mohamed ◽  
Fazil Ahmad ◽  
Ali Alqahtani ◽  
Taha Lqahtani ◽  
Venkatesan Krishna Raju ◽  
...  

This study investigates the complex of curcumin (CMN), which has enhanced solubility and hence, higher cytotoxicity compared to free CMN. Insilco molecular modelling and phase solubility (PS) studies were performed with the drug and carriers for interaction. The complex was characterized by in vitro drug release, FT-IR, PXRD, TGA, DSC, SEM, DLS, and functionalized dyeing test. The result showed that the CMN-PEG6000 complex produced significant properties of solubility (≈ 190 folds) and dissolution (80.68 % at 30 min), with stability constants equivalent to 309 and 377 M-1 at 25 and 37 °C, respectively. It exhibited AL type of isotherm indicating 1:1 stoichiometry. The result from the in vitro cytotoxicity showed that 50 % inhibition (IC50) was achieved on the SW480 and Caco-2 cells at an amount of complex that was considerably lesser than free CMN. Apoptosis study showed that the cells underwent cell death mainly by apoptosis with a small number by necrosis. HIGHLIGHTS Enhanced curcumin solubility up to 190 fold higher than pure curcumin was investigated The phase solubility results of curcumin range from 5.7×10-4 M-1 and 7.8×10-4 M-1 at 25 and 37 °C, respectively First time of novel dyeing test was performed with complex of curcumin, signified its solubility This study provides useful approach for obtaining curcumin products with maximum aqueous solubility GRAPHICAL ABSTRACT


2021 ◽  
Vol 22 (8) ◽  
pp. 4077
Author(s):  
Xiao-Lei Qiu ◽  
Zi-Rui Fan ◽  
Yang-Yang Liu ◽  
Ding-Fu Wang ◽  
Shi-Xin Wang ◽  
...  

A self-nanoemulsifying drug delivery system (SNEDDS) was developed to enhance the absorption of heparin after oral administration, in which heparin was compounded with phospholipids to achieve better fat solubility in the form of heparin-phospholipid (HEP-Pc) complex. HEP-Pc complex was prepared using the solvent evaporation method, which increased the solubility of heparin in n-octanol. The successful preparation of HEP-Pc complex was confirmed by differential scanning calorimetry (DSC), Fourier-transform infrared (FT-IR) spectroscopy, NMR, and SEM. A heparin lipid microemulsion (HEP-LM) was prepared by high-pressure homogenization and characterized. HEP-LM can enhance the absorption of heparin after oral administration, significantly prolong activated partial thromboplastin time (APTT) and thrombin time (TT) in mice, and reduce fibrinogen (FIB) content. All these outcomes indicate that HEP-LM has great potential as an oral heparin formulation.


2020 ◽  
Vol 2020 ◽  
pp. 1-14
Author(s):  
Wang Ya-zhen ◽  
Wu Xue-ying ◽  
Di Yu-tao ◽  
Lan Tian-yu ◽  
Zu Li-wu

In this paper, in order to take advantage of the combination between magnetic nano-Fe3O4 and surface modifier, a pH-sensitive drug delivery system that could effectively deliver doxorubicin (DOX) to tumor tissue was constructed. The novel drug delivery system named Fe3O4-TIPTS-g-(PEI-co-PEG) was prepared through three steps. The first step, a surface modifier with the thiol group, thiohydrazide-iminopropyltriethoxysilane surface modifier (named TIPTS), was synthesized for the first time. The second step, Fe3O4-TIPTS was synthesized by treating nano-Fe3O4 with TIPTS. The last step, Fe3O4-TIPTS-g-(PEI-co-PEG) was synthesized in the presence of the Fe3O4-TIPTS, polyethyleneimine (PEI), and polyethylene glycol (PEG) by mercapto-initiated radical polymerization. Among them, magnetic nanoparticles (MNPs) were used as magnetically responsive carriers, PEG was the surface-modifying compound, and PEI was the drug loading site which primary amine reacts with doxorubicin (DOX). Targeted nanoparticles were considerably stabilize in various physiological solutions and exhibited pH-sensitive performance in drug release. Thence, Fe3O4-TIPTS-g-(PEI-co-PEG) is a promising nanocarrier for targeting tumor therapy.


2020 ◽  
Author(s):  
Muhammad Mujtaba ◽  
Bahar Akyauz Yılmaz ◽  
Demet Cansaran-Duman ◽  
Lalehan Akyuz ◽  
Sevcan Yangın ◽  
...  

AbstractSporopollenin-mediated controlled drug delivery has been studied extensively owing to its physicochemical and biological charachteristics. In the present study, sporopollenin was successfully extracted from pollen grains of C. libani and P. nigra followed by the loading of a commonly known anticancer drug Oxaliplatin. Both the drug loading and physicochemical features were confirmed by using light microscopy, FT-IR, SEM and TGA. For the first time, real-time cell analyzer system, xCELLigence, was employed to record the Oxaliplatin-loaded and sporopollenin-mediated cell death (CaCo-2 and Vero cells) in real time. Both the assays confirmed the slow release of Oxaliplatin from sporopollenin for around 40–45 h. The expression of MYC and FOXO-3 genes significantly increased in CaCo2 cell and decreased non-cancerous Vero cell confirming that sporopollenin-mediated controlled release of Oxaliplatin was promoting apoptosis cell death preventing the spread of its negative effects to nearby healthy cells. All the results suggested that C. libani and P. nigra could be suitable candidates for slow delivery of drugs.


2020 ◽  
Vol 11 (1) ◽  
pp. 176-184
Author(s):  
Pooja Mallya ◽  
Gowda D V ◽  
Mahendran B ◽  
Bhavya M V ◽  
Vikas Jain

Targeting of the drug directly to the cells, tissues, or organs with no impact on healthy cells is a challenge. In the current era, it's been made possible by therapeutic interventions. The novel drug delivery systems such as nano particulates, liposomes, aquasomes, phytosomes, dendrimers, nano sponges, nano micelles are developed. Nano micelles are developed for efficient targeting and are currently in trend as therapeutic carriers of water-insoluble drugs. Micelles are self-assembling Nano-sized colloidal particles with a hydrophobic core and hydrophilic shell. Among the micelle-forming compounds, amphiphilic copolymers, i.e., polymers consisting of hydrophobic block and hydrophilic block, are gaining increasing attention. Polymeric micelles possess high stability both in vitro and in vivo with good biocompatibility. Nano micelles are used widely because of the smaller size range of 10 to 100nm, with greater drug loading capacity. Advantages over other dosage forms include solubilization of poorly soluble drugs, sustained release, protection of drugs from degradation and metabolism. The property discussed includes CMC, size, and aggregation number, and stability. CMC is the minimum polymer concentration required for micelle formation. Aggregation number (Nₐ) is the number of polymeric chains required to form micelles, and it ranges between tens to hundreds. Thermodynamic stability is based on size, the optical clarity of solution, viscosity, and surface tension. Kinetic stability accounts for micellar integrity. This review will discuss some recent trends in using micelles as pharmaceutical carriers such as to deliver drugs in conditions such as TB, cancer, ocular complications, etc.


2011 ◽  
Vol 396-398 ◽  
pp. 2193-2197
Author(s):  
Bao Feng Lin ◽  
Wei Wang ◽  
Yan Ming Li ◽  
Xing Quan Liang ◽  
Yu Min Du

Different chitosan carboxylic salts were successfully prepared via a simple way using chitosan and oxalic, fumaric, salicylic acid for the first time. The characterizations of the salts were evaluated by FT-IR, 13C NMR, 1H NMR, elemental analysis, XRD. The solution properties and moisture absorption-retention abilities of the salts were compared with chitosan. The result indicated that chitosan and carboxylic acid were combined with salt bond. The properties of the salts were related to the type of carboxylic acid added and the formation of salt bond. The water-solubility, wetting effect and moisture-retention absorption abilities of the salts were better than chitosan. They therefore have the potential to substitute for chitosan for easy use as coating in food preservation.


Author(s):  
Prabhat Kumar Sahoo ◽  
Neha S.L ◽  
Arzoo Pannu

Lipids are used as vehicles for the preparation of various formulations prescribed for administrations, including emulsions, ointments, suspension, tablets, and suppositories. The first parental nano-emulsion was discovered from the 1950s when it was added to the intravenous administration of lipid and lipid-soluble substances. Lipid-based drug delivery systems are important nowadays. Solid nanoparticles (SLN) and Nanostructured lipid carriers (NLC) are very proficient due to the ease of production process, scale-up capability, bio-compatibility, the biodegradability of formulation components and other specific features of the proposed route. The administration or nature of the materials must be loaded into these delivery systems. The main objectives of this review are to discuss an overview of second-generation nanoparticles, their limitations, structures, and route of administration, with emphasis on the effectiveness of such formulations. NLC is the second generation of lipid nanoparticles having a structure like nanoemulsion. The first generation of nanoparticles was SLN. The difference between both of them is at its core. Both of them are a colloidal carrier in submicron size in the range of 40-1000 nm. NLC is the most promising novel drug delivery system over the SLN due to solving the problem of drug loading and drug crystallinity. Solid and liquid lipids combination in NLC formation, improve its quality as compare to SLN. NLC has three types of structures: random, amorphous, and multiple. The random structure containing solid-liquid lipids and consisting crystal and the liquid lipid irregular in shape; thereby enhance the ability of the lipid layer to pass through the membrane. The second is the amorphous structure. It is less crystalline in nature and can prevent the leakage of the loaded drug. The third type is multiple structures, which have higher liquid lipid concentrations than other types. The excipients used to form the NLC are bio-compatible, biodegradable and non-irritating, most of which can be detected using GRAS. NLC is a promising delivery system to deliver the drug through pulmonary, ocular, CNS, and oral route of administration. Various methods of preparation and composition of NLC influence its stability Parameters. In recent years at the educational level, the potential of NLC as a delivery mechanism targeting various organs has been investigated in detail.


2019 ◽  
Vol 26 (14) ◽  
pp. 2502-2513 ◽  
Author(s):  
Md. Iqbal Hassan Khan ◽  
Xingye An ◽  
Lei Dai ◽  
Hailong Li ◽  
Avik Khan ◽  
...  

The development of innovative drug delivery systems, versatile to different drug characteristics with better effectiveness and safety, has always been in high demand. Chitosan, an aminopolysaccharide, derived from natural chitin biomass, has received much attention as one of the emerging pharmaceutical excipients and drug delivery entities. Chitosan and its derivatives can be used for direct compression tablets, as disintegrant for controlled release or for improving dissolution. Chitosan has been reported for use in drug delivery system to produce drugs with enhanced muco-adhesiveness, permeation, absorption and bioavailability. Due to filmogenic and ionic properties of chitosan and its derivative(s), drug release mechanism using microsphere technology in hydrogel formulation is particularly relevant to pharmaceutical product development. This review highlights the suitability and future of chitosan in drug delivery with special attention to drug loading and release from chitosan based hydrogels. Extensive studies on the favorable non-toxicity, biocompatibility, biodegradability, solubility and molecular weight variation have made this polymer an attractive candidate for developing novel drug delivery systems including various advanced therapeutic applications such as gene delivery, DNA based drugs, organ specific drug carrier, cancer drug carrier, etc.


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