scholarly journals Synthesis of a novel green carbon dots as a bioimaging agent and a drug delivery system for enhanced antioxidant and antibacterial efficacy

2020 ◽  
Author(s):  
Neeraj Tejwan ◽  
Mousumi Kundu ◽  
Anirudh Sharma ◽  
Joydeep Das ◽  
Parames C Sil

Abstract Background Now-a-days, synthesis of carbon dots (CDs) from renewable sources has attracted considerable attention due to their wide spread availability, lower cost, higher aqueous solubility and more biocompatibility. Here, we have synthesized water soluble CDs from the root extract of red Korean ginseng via simple microwave irradiation. The CDs were further loaded with a natural flavonoid, rutin, to check its efficacy as a drug delivery system. Result The CDs showed a size distribution between 1–4 nm and excitation-dependent fluorescence emission, and could be used as a bio-imaging agent.The CDs showed a drug loading content of 14% and a sustained drug release behavior at physiological conditions. CDs showed excellent free radical scavenging activity both in cell free systems and intra-cellular conditions. Besides, loading with the drug further improved the intra-cellular radical scavenging activity. The CDs and the nanohybrids also showed very little toxicity upto the concentration of 100 µg/mL in normal kidney epithelial cells. The CDs and the nanohybrids also showed a dose-dependent antibacterial effect against both gram negative as well as gram positive bacteria. Conclusion Our synthesized green CDs can be considered as a promising candidate for the biomedical applications due to its facile synthesis, low cytotoxicity, excellent fluorescent properties and potential as drug delivery systems.

2021 ◽  
Vol 11 (2) ◽  
pp. 95-102
Author(s):  
Mohammed Waseem A ◽  
Ajin P Kurian ◽  
Dhanapal Y

Objective: The purpose of this study was to develop salmeterol, fluticasone nano-lipid carriers to estimate as potentials of oral delivery system for poorly water soluble drugs. Nano-lipid carriers applied to chronomodulated pulsatile drug delivery system maintain the concentration level by releasing the drug at predetermined time interval throughout the management of asthma. Method: The particle size analysis revealed that all the formulations were within the nanometer range of 150.0±2.4nm. Percentage of entrapment efficiency and drug loading were found to be 69.5±4.4 - 85.3±1.3 and 9.358±2.2-10.45±8.1, respectively. The SLM-FCN nano-lipid carrier’s optimized formulation showed spherical morphology with smooth surface under the transmission electron microscope (TEM), the crystalline characterization of drug in NLC was investigated by X-ray diffraction and differential scanning calorimetric (DSC). The ex-vivo permeation study showed many folds increment in the SLM-FCN NLCs compared to powder SLM-FCN 96.0±2.55 and pulsing plugs in-vivo drug released effectively in pre-determine time intervals. Conclusion: The progression concludes that chronomodulated programming pulsatile release was achieved with modified pulsing bilayerd plugged of salmeterol, fluticasone propionate NLCs, formulation remarkably improved oral bioavailability. we promise that finding in this investigations suggest practicability of the dosage form system can be taken after at bedtime then it will be delivered in the early morning which maintains the drug concentration throughout to control asthma.


INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (10) ◽  
pp. 49-54
Author(s):  
M. Gohel ◽  
◽  
R. Kureshi ◽  
L Hingorani ◽  
A. Patel ◽  
...  

Withaferin A, a steroidal lactone which is present in dry root extract of Withania somnifera (WSE), is reported to possess numerous pharmacological activities and shows poor aqueous solubility. The purpose of this study is to enhance the dissolution rate and oral bioavailability of WSE by incorporating it in self nano emulsifying drug delivery system (SNEDDS). Capmul MCM-based SNEDDS formulation with Tween 20 as surfactant and ethanol as co surfactant was developed for oral delivery of withaferin A. Optimised SNEDDS was evaluated for its self-emulsification time and viscosity, droplet size. The optimised SNEDDS formulation containing withaferin A, Capmul MCM(12.4%), Tween 20 (58.2%) and ethanol (29%), and showed higher in vitro drug release as compared to pure WSE. These results demonstrate the potential use of SNEDDS for improving the oral bioavailability of poor water soluble compounds such as withaferin A.


Author(s):  
Vikrant P Wankhade ◽  
Nivedita S Kale ◽  
K.K Tapar

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.


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.


RSC Advances ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 2656-2663
Author(s):  
Boye Zhang ◽  
Qianqian Duan ◽  
Yi Li ◽  
Jianming Wang ◽  
Wendong Zhang ◽  
...  

The system is pH-responsive and redox-controlled release. And the charge reversal and size transitions of the system can enhance the targeted ability. Moreover, the system can recognize the cancer cells by the fluorescence imaging.


2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Vijayakumar Sundaram ◽  
Selvaraju Sadhasivam ◽  
Sivaraj Chandrasekaran ◽  
Raaman Nanjian ◽  
Arjun Pandian

Abstract Background Strobilanthes heyneanus (Nilgirianthus heyneanus) belongs to the family Acanthaceae that contains many species with potential for diverse medicinal uses. It is also called ‘Karun kurinji’ and is commonly found in the South-West regions of India. The species are commonly used in rheumatic complaints, sprain of the ankle, and hernia. The objectives of the study were to evaluate the antioxidant activity, phytochemical analysis, and antibacterial activities of the root extract of S. heyneanus. Results The radical scavenging and reduction assays such as DPPH● radical and OH● radical scavenging assays, as well as phosphomolybdenum reduction and Fe3+ reducing power assays, were determined for the root extract. The highest DPPH● radical scavenging activity was 88.23 ± 1.32 at 120 μg/mL concentration, and the calculated IC50 was 38.52 μg/mL concentration. The highest OH● radical scavenging activity was 51.28 ± 1.06 at 120 μg/mL concentration, and the calculated IC50 was 51.28 μg/mL concentration. The highest ABTS●+ radical scavenging activity was 91.28 ± 1.12 at 30 μg/mL concentration, and the calculated IC50 was 33.92 μg/mL concentration. The highest phosphomolybdenum reduction was 87.43 ± 0.90 at 120 μg/mL concentration, and the calculated RC50 was 24.74 μg/mL concentration. The highest Fe3+ reduction was 89.38 ± 0.98 at 120 μg/mL concentration, and the calculated RC50 was 31.06 μg/mL concentration. The antibacterial activity of S. heyneanus showed the highest zone of inhibition of 24 mm for Salmonella typhi with 500 μg/mL concentration. The cytotoxicity limits of the root extracts were tested by MTT assay using human dermal fibroblast cell lines, reflecting > 90% cell viability at a concentration of 500 μg/mL. Conclusions The current study showed that the root extract of S. heyneanus has better antioxidant properties and potential anti-bacterial compounds. The phytochemical analysis of the root extract showed the presence of alkaloids, steroids, terpenoids, phenols, flavonoids, tannins, saponins, glycosides, and carbohydrates, which are responsible for the antibacterial root extract of S. heyneanus synergistically.


Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  


Author(s):  
Kanuri Lakshmi Prasad ◽  
Kuralla Hari

Objective: To enhance solubility and dissolution rate of budesonide through development of solid self-nanoemulsifying drug delivery system (S-SNEDDS). Methods: Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) were prepared and ternary phase diagram was constructed using Origin pro 8. Liquid self-nanoemulsifying formulation LF2 having 20% oil and 80% of surfactant/co-surfactant was optimized from the three formulations (LF1-LF3) to convert in to solid, through various characterization techniques like self-emulsification, in vitro drug release profile and drug content estimation. The prepared L-SNEDDS converted into S-SNEDDS, SF1-SF6 by adsorption technique using Aerosil 200, Neusilin US2, and Neusilin UFL2 to improve flowability, compressibility and stability. Results: Formulation LF2 exhibited globule size of 82.4 nm, PDI 0.349 and Zeta potential -28.6 mV with drug indicating the stability and homogeneity of particles. The optimized formulation SF4 containing Neusilin UFL2 was characterized by DSC, FTIR, X-Ray diffraction studies and found no incompatibility and no major shifts were noticed. Formulation SF4 released 100 % drug in 20 min against pure drug release of 47 % in 60 min. Regardless of the form (i.e. liquid or solid) similar performance of emulsification efficiency is observed. Conclusion: The results demonstrated that the technique of novel solid self-nanoemulsifying drug delivery system can be employed to enhance the solubility and dissolution rate of poorly water-soluble drug budesonide.


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