Moxifloxacin Loaded Polymeric Nanoparticles for Sustained Ocular Drug Delivery

2012 ◽  
Vol 5 (2) ◽  
pp. 1727-1734
Author(s):  
A P Gadad ◽  
Sharath Chandra P ◽  
Dandagi P M ◽  
V S Mastiholimath
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Glycolic Acid ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Eye Drops ◽  
Potential Drug ◽  
Sustained Effect ◽  
Drug Entrapment Efficiency

Efficient drug delivery to the ocular region is a challenging goal. Only a very small amount (about l-3%) of the dosage actually penetrates through the cornea and reaches intraocular tissues. To overcome these problems of conventional dosage forms, novel drug delivery systems like nanoparticles were designed. Moxifloxacin-loaded poly (lactic-co-glycolic acid) nanosuspension was prepared with the aim of providing sustained effect for ocular delivery for 24 hours. Nanosuspensions were prepared by nanoprecipitation method using poly(lactic-co-glycolic acid) and evaluated for particle size, surface morphology, zeta potential, drug entrapment efficiency, in vitro release and ex vivo transcorneal permeability, and were compared with marketed products. Microbiological efficacy was tested against Staphylococcus aureus and Pseudomonas aeroginosa using cup plate method. Spherical uniform particles (202.5 nm) with a polydispersity index of 0.226 and negative zeta potential (– 25.45 mV) were obtained for MF4 (drug to polymer ratio 1:0.4). Drug entrapment efficiency for MF4 was found to be 83.1%. The cumulative percent drug release for formulation MF4 after 24 hours was 86.1%, showing a sustained effect in controlling the bacterial conjunctivitis thereby avoiding frequent administration of dosage. MFX-loaded PLGA nanoparticles (MF4) showed a significantly higher drug permeation capability compared to the commercial marketed eye drops in ex vivo transcorneal permeation studies and also showed better antimicrobial efficacy compared to the marketed formulation. The results indicate that Moxifloxacin-loaded PLGA nanosuspension could be utilized as a potential drug delivery system for sustained release in ophthalmic application.

Formulation and evaluation of resveratrol loaded cubosomal nanoformulation for topical delivery

2020 ◽  
Vol 17 ◽  
Author(s):  
Bhaskar Kurangi ◽  
Sunil Jalalpure ◽  
Satveer Jagwani
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Topical Application ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Drug Permeation

Aim: The aim of the study was to formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC) through topical application. Background: Resveratrol (RV) is a nutraceutical compound that has exciting pharmacological potential in different diseases including cancers. Many studies of resveratrol have been reported for anti-melanoma activity. Due to its low bioavailability, the activities of resveratrol are strongly limited. Hence, an approach with nanotechnology has been done to increase its activity through transdermal drug delivery. Objective: To formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC). To evaluate resveratrol-loaded cubosomal gel (RC-Gel) for its topical application. Methods: RC was formulated by homogenization technique and optimized using a 2-factor 3-level factorial design. Formulated RCs were characterized for particle size, zeta potential, and entrapment efficiency. Optimized RC was evaluated for in vitro release and stability study. Optimized RC was further formulated into cubosomal gel (RC-Gel) using carbopol and evaluated for drug permeation and deposition. Furthermore, developed RC-Gel was evaluated for its topical application using skin irritancy, toxicity, and in vivo local bioavailability studies. Results: The optimized RC indicated cubic-shaped structure with mean particle size, entrapment efficiency, and zeta potential were 113±2.36 nm, 85.07 ± 0.91%, and -27.40 ± 1.40 mV respectively. In vitro drug release of optimized RC demonstrated biphasic drug release with the diffusion-controlled release of resveratrol (RV) (87.20 ± 2.25%). The RC-Gel demonstrated better drug permeation and deposition in mice skin layers. The composition of RC-Gel has been proved non-irritant to the mice skin. In vivo local bioavailability study depicted the good potential of RC-Gel for skin localization. Conclusion: The RC nanoformulation proposes a promising drug delivery system for melanoma treatment simply through topical application.

scholarly journals Preparation and physicochemical characterization of Eudragit® RL100 Nanosuspension with potential for Ocular Delivery of Sulfacetamide

2010 ◽  
Vol 13 (4) ◽  
pp. 510 ◽  
Author(s):  
Bivash Mandal ◽  
Kenneth S Alexander ◽  
Alan T Riga
Keyword(s):  
Zeta Potential ◽  
Bacterial Infections ◽  
Room Temperature ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
Freeze Dried ◽  
Drug Entrapment Efficiency

Purpose: Polymeric nanosuspension was prepared from an inert polymer resin (Eudragit® RL100) with the aim of improving the availability of sulfacetamide at the intraocular level to combat bacterial infections. Methods: Nanosuspensions were prepared by the solvent displacement method using acetone and Pluronic® F108 solution. Drug to polymer ratio was selected as formulation variable. Characterization of the nanosupension was performed by measuring particle size, zeta potential, Fourier Transform infrared spectra (FTIR), Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD), drug entrapment efficiency and in vitro release. In addition, freeze drying, redispersibility and short term stability study at room temperature and at 40C were performed. Results: Spherical, uniform particles (size below 500 nm) with positive zeta potential were obtained. No significant chemical interactions between drug and polymer were observed in the solid state characterization of the freeze dried nanosuspension (FDN). Drug entrapment efficiency of the selected batch was increased by changing the pH of the external phase and addition of polymethyl methacrylate in the formulation. The prepared nanosuspension exhibited good stability after storage at room temperature and at 40C. Sucrose and Mannitol were used as cryoprotectants and exhibited good water redispersibility of the FDN. Conclusion: The results indicate that the formulation of sulfacetamide in Eudragit® RL100 nanosuspension could be utilized as potential delivery system for treating ocular bacterial infections.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF PIPER RETROFRACTUM EXTRACT LOADED MUCOADHESIVE NANOSTRUCTURED LIPID CARRIERS FOR TOPICAL ORAL DRUG DELIVERY

2017 ◽  
Vol 9 (9) ◽  
pp. 79
Author(s):  
Kavee Srichaivatana ◽  
Anan Ounaroon ◽  
Waree Tiyaboonchai
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Oral Cavity ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Oral Drug ◽  
Drug Entrapment Efficiency ◽  
Piper Retrofractum

Objective: To develop and characterize Piper retrofractum extract loaded nanostructured lipid carriers (PRE loaded NLCs) for topical oral cavity administration to enhance bioavailability and stability of piperine.Methods: PRE loaded NLCs were prepared with a hot high-pressure homogenization technique followed by coating the particle surface with mucoadhesive polymers; polyethene glycol 400 (PEG) and polyvinyl alcohol (PVA). The physicochemical properties in terms of particle size, polydispersity index, zeta potential, drug entrapment efficiency, in vitro drug release profile and antimicrobial activities were examined. In vitro, mucoadhesion studies were assessed by the wash-off test. The physicochemical stabilities of mouth spray containing PRE loaded NLCs were investigated by kept at room temperature and 4 °C for 6 mo.Results: The PRE loaded NLCs showed spherical shape with a mean particle size of ~100-120 nm and zeta potential of ~-24 mV. Up to 90% drug entrapment efficiency was achieved. PEG-NLCs and PVA-NLCs showed a strong interaction with porcine buccal mucosa than uncoated-NLCs. All PRE loaded NLCs formulations revealed fast release characteristics and effective against Streptococcus mutans and S. sanguinis. The mouth spray containing PRE loaded NLCs showed good physical stability without particle aggregation. In addition, the chemical stability of piperine in NLCs was significantly improved during storage at both storage conditions compared to its solution form.Conclusion: The developed PRE loaded polymer coated-NLCs showed high potential to use as a local drug delivery system for reducing the bacterial growth in the oral cavity.

scholarly journals OPTIMIZATION AND CHARACTERIZATION OF DOXORUBICIN LOADED SOLID LIPID NANOSUSPENSION FOR NOSE TO BRAIN DELIVERY USING DESIGN EXPERT SOFTWARE

2021 ◽  
pp. 45-57
Author(s):  
VIRAG A. SHAH ◽  
JAYVADAN K. PATEL
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
High Speed ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Brain Targeting ◽  
Solid Lipid ◽  
Stirring Time

Objective: The goal of the current study was to investigate the possible use of solid lipid nanosuspension (SLNs) as a drug delivery method to boost doxorubicin (DOX) brain-targeting performance after intranasal (i. n.) administration.  Methods: 33 factorial design was applied for optimization by using lipid concentration, surfactant concentration, and High-speed homogenizer (HSH) stirring time as dependent variables, and their effect was observed on particles size, Polydispersity index (PDI), and entrapment efficiency.  Results: With the composition of Compritol® 888 ATO (4.6 % w/v), tween 80 (1.9 % w/v), and HSH stirring time, the optimized formula DOX-SLNs prepared (10 min). Particle size, PDI, zeta potential, entrapment efficiency, percent in vitro release were found to be 167.47±6.09 nm, 0.23±0.02, 24.1 mV, 75.3±2.79, and 89.35±3.27 percent in 24 h, respectively, for optimized formulation (V-O). No major changes in particle size, zeta potential, and entrapping efficiency were found in the stability studies at 4±2 °C (refrigerator) and 25±2 °C/60±5% RH up to 3 mo.  Conclusion: Following the non-invasive nose-to-brain drug delivery, which is a promising therapeutic strategy, the positive findings confirmed the current optimized DOX-loaded SLNs formulation.

Nifedipine-Loaded Polymeric Nanocapsules: Validation of a Stability-Indicating HPLC Method to Evaluate the Drug Entrapment Efficiency and In Vitro Release Profiles

2013 ◽  
Vol 96 (2) ◽  
pp. 276-281 ◽  
Author(s):  
Andréa Granada ◽  
Monika Piazzon Tagliari ◽  
Valdir Soldi ◽  
Marcos Antônio Segatto Silva ◽  
Betina Ghiel Zanetti-Ramos ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Hplc Method ◽  
Stability Indicating ◽  
Polymeric Nanocapsules ◽  
Drug Entrapment Efficiency ◽  
High Entrapment Efficiency

Abstract A simple stability-indicating analytical method was developed and validated to quantify nifedipine in polymeric nanocapsule suspensions; an in vitro drug release study was then carried out. The analysis was performed using an RP C18 column, UV-Vis detection at 262 nm, and methanol–water (70 + 30, v/v) mobile phase at a flow rate of 1.2 mL/min. The method was validated in terms of specificity, linearity and range, LOQ, accuracy, precision, and robustness. The results obtained were within the acceptable ranges. The nanocapsules, made of poly(ε-caprolactone), were prepared by the solvent displacement technique and showed high entrapment efficiency. The entrapment efficiency was 97.6 and 98.2% for the nifedipine-loaded polymeric nanocapsules prepared from polyvinyl alcohol (PVA) and Pluronic F68 (PF68), respectively. The particle size and zeta potential of nanocapsules were found to be influenced by the nature of the stabilizer used. The mean diameter and zeta potential for nanocapsules with PVA and PF68 were 290.9 and 179.9 nm, and –17.7 mV and –32.7 mV, respectively. The two formulations prepared showed a drug release of up to 70% over 4 days. This behavior indicates the viability of this drug delivery system for use as a controlled-release system.

Development of lipid-based microsuspensions for improved ophthalmic delivery of gentamicin sulphate

2021 ◽  
Author(s):  
Adaeze Linda Onugwu ◽  
Chinazom Precious Agbo ◽  
Chinekwu Sherridan Nwagwu ◽  
Samuel Emeka Uzondu ◽  
Adaeze Chidiebere Echezona ◽  
...  
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Eye Drops ◽  
Ex Vivo Permeation ◽  
Anterior Eye Segment ◽  
Ophthalmic Delivery ◽  
Gentamicin Sulphate ◽  
High Entrapment Efficiency

Aim: Anterior eye segment disorders are treated with eye drops and ointments, which have low ocular bioavailability necessitating the need for improved alternatives. Lipid microsuspension of gentamicin sulphate was developed for the treatment of susceptible eye diseases. Materials & methods: Lipid microsuspensions encapsulating gentamicin sulphate were produced by hot homogenization and evaluated. Ex vivo permeation and ocular irritancy tests were also conducted. Results & conclusion: Stable microsuspensions with high entrapment efficiency and satisfactory osmolarities were obtained. Release studies achieved 49–88% in vitro release at 12 h with sustained permeability of gentamicin compared with conventional gentamicin eye drop (Evril®). No irritation was observed following Draize’s test. The microsuspensions have great potential as ocular delivery system of gentamicin sulphate.

scholarly journals EFFECT OF PEGYLATED EDGE ACTIVATOR ON SPAN 60 BASED- NANOVESICLES: COMPARISON BETWEEN MYRJ 52 AND MYRJ 59

2019 ◽  
Author(s):  
Elsaied H. Elsaied ◽  
Hamdy M Dawaba ◽  
El Sherbini A Ibrahim ◽  
Mohsen I Afouna
Keyword(s):  
Polyethylene Glycol ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Potential Drug ◽  
Span 60 ◽  
Surface Modified ◽  
Vitro Release ◽  
Edge Activator

In recent years, Span 60 based nanovesicles have been the object of growing scientific attention as an alternative potential drug delivery system to conventional liposomes. Surface modification of nanovesicles can adjust the drug release rate and the affinity for the target site. The aim of present work was firstly to study the effects of different PEGylated edge activator (Myrj 52 and Myrj 59) on Span 60 based nanovesicles. Nanovesicles were prepared using Span 60 alone or in combination with Myrj 52 (polyethylene glycol 2000 monostearate) or Myrj 59 (polyethylene glycol 4400 monostearate) by employing the ethanol injection method. Myrj 52and Myrj 59 are hydrophilic nonionic surfactants were used to modify the surface of the developed vesicles. Dynamic light scattering was used to determine the size, zeta potential and polydispersity index of the nanovesicles formulation. The vesicles were also characterized for entrapment efficiency and in vitro release. In current work, the modified nanovesicles size (ranging from 54.32 to 141.7 nm), zeta potential (ranging from -5.67 to -27.1 mV) and polydispersity index (ranging from0.248 to 0.531) indicated that the surface modified nanovesicles vesicles are a homogenous and mono-disperse nanovesicles dispersions. The non-modified nanovesicles are showed higher particles size (>2 times) compared to modified nanovesicles. The modified nanovesicles were showed entrapment efficiency ranging from 36.42 to 78.13 %. All the modified nanovesicles showed accepted in vitro release of TN from nanovesicles (>70% released after 8 h), followed Higuchi models as drug release mechanism. In conclusion, these surface modified nanovesicles could be used as a potential drug carrier for a variety of drugs.

scholarly journals Preparation of In Situ Cross-Linked N-Maleoyl Chitosan-Oxidized Sodium Alginate Hydrogels for Drug Delivery Applications

2019 ◽  
Vol 7 (21) ◽  
pp. 3546-3553
Author(s):  
Subur P. Pasaribu ◽  
Jamaran Kaban ◽  
Mimpin Ginting ◽  
Jansen Silalahi
Keyword(s):  
Drug Delivery ◽  
Schiff Base ◽  
Sodium Alginate ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Drug Entrapment Efficiency ◽  
Drug Delivery Applications ◽  
Release Profiles

AIM: This study was aimed to prepare in situ cross-linked N-maleoyl chitosan – oxidised sodium alginate (MCS – OSA) hydrogel loaded with metronidazole (MTZ) for drug delivery applications. METHODS: The hydrogel was prepared by in situ cross-linking via Schiff base reaction between amine (-NH2) groups from MCS and aldehyde (-CHO) groups from OSA at the different ratio, and the MTZ was loaded into the hydrogels along with the gelatin processes. RESULTS: The highest drug entrapment efficiency (DEE) was exhibited by MTZ-H3 (5: 5) with DEE of 99.20% and a gel fraction of 97.52%. FTIR results revealed that Schiff base reaction was occurred by the absorption peak of –C = N- groups at 1628 cm-1 and indicated that there is insignificant alteration at different ratio of MCS and OSA. The best sustained of in vitro release profiles of MTZ was shown by MTZ-H3, which is 74.92% and 75.65% at pH 1.2 and 7.4 for 12 h of release, respectively. CONCLUSION: The optimised ratio between MCS and OSA to prepare in situ cross-linked hydrogels were found to be 5:5 according to the results of DEE and in vitro drug release profiles of MTZ and the MTZ loaded MCS-OSA hydrogels have a great potential which can be applied in biomedical applications.

scholarly journals Solid nanostructured lipid carriers loaded with silymarin for oral delivery: Formulation development and evaluation

2021 ◽  
Vol 3 (4) ◽  
pp. 56-67
Author(s):  
Rajashree Hirlekar ◽  
Esha Patil ◽  
Srinivas Bhairy
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Drug Loading ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Formulation Development ◽  
Ex Vivo Permeation

The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of silymarin loaded nanostructured lipid carriers (NLCs). The prepared silymarin loaded NLCs and DANs were characterized for various quality parameters. Silymarin loaded NLCs were prepared by a modified hot melt emulsification ultra-sonication method using glyceryl monostearate (GMS), capmul MCM C8 EP (CAP) and gelucire 50/13 (G50/13) as solid lipid, liquid lipid and surfactant respectively. For better stability, NLC dispersion was converted into DANs by adsorbing them onto some suitable carriers. NLCs and DANs were characterized for particle size, polydispersity index, zeta potential, entrapment efficiency, drug loading, assay, thermal behavior, crystallinity and morphological study. The optimized NLCs have a mean particle size of 206.1±012.5 nm (size distribution of 0.249±0.058), a zeta potential of -32.5±1.2 mV with high entrapment of 95.60±0.45% and drug loading of 1.90±0.08%. The X-ray diffraction and endothermic peaks confirmed the maximum encapsulation of active in lipid matrices. The particles were spherical with smooth surface morphology. In-vitro release studies showed sustained drug release for up to 24 h. Ex-vivo permeation in the presence and absence of lymphatic blocker indicates the uptake of silymarin loaded NLCs by the lymphatic route. Silymarin loaded NLCs prepared had a nanosize distribution with high entrapment efficiency. The ex-vivo permeation study for optimized NLC formulation exhibited the lymphatic uptake of active. Dispersion stability was increased by preparing the DANs. The solid dry powder is used for oral reconstitution and can be further converted into tablets or filled into capsules.

scholarly journals Niosomal Nanocarriers for Enhanced Skin Delivery of Quercetin with Functions of Anti-Tyrosinase and Antioxidant

Molecules ◽  
2019 ◽  
Vol 24 (12) ◽  
pp. 2322 ◽  
Author(s):  
Banyi Lu ◽  
Yanting Huang ◽  
Zhongyun Chen ◽  
Jingyi Ye ◽  
Hongyu Xu ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Ex Vivo ◽  
Radical Scavenging ◽  
Entrapment Efficiency ◽  
Potential Range ◽  
Skin Delivery ◽  
Antioxidant Capacities ◽  
Drug Entrapment Efficiency ◽  
Skin Retention

This study aimed to screen an effective flavonoid with promising whitening and antioxidant capacities, and design flavonoid-loaded niosomes to improve its solubility, stability, and penetration. In vitro anti-tyrosinase and 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging experiments were conducted to investigate the whitening and antioxidant capacities of several flavonoids, including quercetin, morin, festin, myricetin, rutin, and breviscapine. The conductivity, viscosity, and particle size of Span60-RH40-based formulation of nonionic surfactant vesicles (niosomes) with different mass ratios were studied to determine the most appropriate formulation. Drug-loaded niosomes were characterized for size, zeta potential, morphology, and entrapment efficiency. The photostability, solubility, release behavior, ex vivo drug penetration, and skin retention were also studied. The results showed that quercetin has considerable whitening and antioxidant capacities and Span60-RH40 at a mass ratio of 9:11 forms spherical or oval niosomes of 97.6 ± 3.1 nm with a zeta potential range of 31.1 ± 0.9 mV, and drug entrapment efficiency as high as 87.3 ± 1.6%. Niosomes remarkably improved the solubility and photostability of quercetin. Furthermore, compared to quercetin solution, quercetin-niosomes had the advantages of sustained release and improved transdermal penetration, with skin retention 2.95 times higher than quercetin solution.

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