FORMULATION AND CHARACTERIZATION OF RITONAVIR LOADED PRONIOSOMES FOR ORAL DRUG DELIVERY

Proniosomes of ritonavir were prepared by slurry method using Span 60, maltodextrin and cholesterol. The ratio of concentration of Span 60 to cholesterol was altered while keeping concentration of drug and maltodextrin constant. Prepared formulations were studied for micromeritic properties, entrapment efficiency, particle size, surface morphology and in vitro drug release. Micromeritic properties of all formulations increased as compared to drug and carrier alone. Entrapment efficiency was observed greater than 90 % and drug release was found to be sustained for upto 12 hours in case of all formulations. Pure drug, carrier and optimized batch F2 was further characterized for SEM, DSC, XRD. Results revealed transformation of crystalline drug to amorphous state. Stability studies performed at refrigeration and room temperature showed that proniosomes were stable at both the temperatures. It is concluded that proniosomes act as efficient and promising carrier system for ritonavir.

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Facile Synthesis of Chitosan Based-(AMPS-co-AA) Semi-IPNs as a Potential Drug Carrier: Enzymatic Degradation, Cytotoxicity, and Preliminary Safety Evaluation

Current Drug Delivery ◽

10.2174/1567201815666181024152101 ◽

2019 ◽

Vol 16 (3) ◽

pp. 242-253 ◽

Cited By ~ 2

Author(s):

Kaleem Ullah ◽

Muhammad Sohail ◽

Abdul Mannan ◽

Haroon Rashid ◽

Aamna Shah ◽

...

Keyword(s):

Drug Release ◽

Oral Drug Delivery ◽

Drug Carrier ◽

Drug Loading ◽

In Vitro Cytotoxicity ◽

Oral Drug ◽

Specific Enzyme ◽

Oral Toxicity ◽

Scanning Calorimetry

Objective: The study describes the development of chitosan-based (AMPS-co-AA) semi-IPN hydrogels using free radical polymerization technique. Methods: The resulting hydrogels were characterized using Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC), X-Ray diffraction (XRD), and Scanning Electron Microscopy (SEM). The successful crosslinking of chitosan, 2- Acrylamido-2-Methylpropane Sulfonic Acid (AMPS), and Acrylic Acid (AA) was confirmed by FT IR. Unloaded and drug-loaded hydrogels exhibited higher thermal stability after crosslinking compared to the individual components. XRD confirmed the decrease in crystallinity after hydrogel formation and molecular dispersion of Oxaliplatin (OXP) in the polymeric network. SEM showed rough, vague and nebulous surface resulting from crosslinking and loading of OXP. Results: The experimental results revealed that swelling and drug release were influenced by the pH of the medium being low at acidic pH and higher at basic pH. Increasing the concentration of chitosan and AA enhanced the swelling, drug loading and drug release while AMPS was found to act inversely. Conclusion: It was confirmed that the hydrogels were degraded more by specific enzyme lysozyme as compared to the non-specific enzyme collagenase. In-vitro cytotoxicity suggested that the unloaded hydrogels were non-cytotoxic while crude drug and drug-loaded hydrogel exhibited dose-dependent cytotoxicity against HCT-116 and MCF-7. Results of acute oral toxicity on rabbits demonstrated that the hydrogels are non-toxic up to 3900 mg/kg after oral administration, as no toxicity or histopathological changes were observed in comparison to control rabbits. These pH-sensitive hydrogels appear to provide an ideal basis as a safe carrier for oral drug delivery.

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Formulation and Evaluation of Controlled Release Maintenance Dose Loaded Niosomes of Anti-Hypertensive Drug

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2019.110605 ◽

2019 ◽

Vol 11 (06) ◽

Author(s):

Chandani Makvana ◽

Satyajit Sahoo

Keyword(s):

Controlled Release ◽

Drug Release ◽

Zeta Potential ◽

Drug Carrier ◽

Entrapment Efficiency ◽

Drug Carriers ◽

Vesicle Size ◽

Drug Content ◽

Span 60

The present study was aimed to formulate, comparatively evaluate and optimize multiple lipid drug carriers of valsartan for oral controlled release to overcome the problems associated with the drug such as bioavailability, to reduce the dosage regimen, half life and to determine the appropriateness of niosomal formulation as a drug carrier. Ether injection method was chosen for the formulation of physically and chemically stable niosomes of valsartan. The formulation and process parameters were optimized by manufacturing placebo niosomes. Than drug loaded niosome was prepared by varying the concentration of span 60. The prepared nine formulations were evaluated for various parameters. Placebo niosomes were evaluated for appearance, odour, texture, creaming volume, pH and changes after 15 days. The medicated nine formulations were evaluated for organoleptic properties (appearance/color, odour), pH, total drug content, entrapment efficiency, mean particle size and polydispersibility index, zeta potential and In-vitro drug release. All formulations were off-white in color, odourless, and fluid in nature. It was stable and did not show sedimentation. The pH was found to be in the range of 4.6-5.4. Drug content was found in the range of 89.13 to 99.52. The Entrapment efficiency was found in range of 79.05 to 98.24. The mean vesicle size of drug loaded niosomes of the different batches ranged between 2.52-3.42μm. The polydispersvity index was in the range of 0.325 to 0.420 which indicates a narrow vesicle size distribution. The values of zeta potential were in the range of -20.29 mV to -30.55 mV which indicates that niosome had sufficient charge and mobility to inhibit aggregation of vesicles. All the nine formulations shows constant drug release in controlled manner up to 24 h. Formulation V7 was considered to be the best formulation as the % drug content (99.52 ± 0.97), % entrapment efficiency (98.24 ± 1.50) and % drug release at the end of 24th h (98.55) were high for V7. The optimized formulation V7 showed higher degree of correlation coefficient (r2) 0.9805 which indicates process of constant drug release from dosage form. The present study concludes that the prepared niosome is a convenient and efficiency carrier for the delivery of antihypertensive drug. Besides this, it provided controlled delivery of drug.

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Development and Characterization of Elastic Liposomes of Metronidazole for the Treatment of Bacterial Infection

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v10i6-s.4454 ◽

2020 ◽

Vol 10 (6-s) ◽

pp. 83-88

Author(s):

Priyam Chaurasiya ◽

Ritesh Agarwal ◽

Kavita R. Loksh

Keyword(s):

Drug Release ◽

Release Kinetics ◽

Entrapment Efficiency ◽

Topical Administration ◽

Stability Study ◽

Vesicle Size ◽

Rotary Evaporation ◽

Span 60

Objective: The objective of present study is to develop and evaluate the elastic liposomes of metronidazole so as to provide the sustained release and improve its bioavailability. Methods: Elastic liposomes were prepared by rotary evaporation method using Span 80 and Span 60 as a surfactants. The prepared elastic liposomes were evaluated for entrapment efficiency, vesicle size, In vitro drug release. Results: The drug release profiles from different elastic liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. The formulation prepared showed an average vesicle size 185.4nm. The amount of drug entrapped into the elastic liposomes formulations was determined. The entrapment efficiency was found to be 73.45±0.78 %. A good amount of drug was entrapped in the liposome formulations prepared. Based on different parameters formulations of batch TG2 was found to be the best formulations. Stability study was performed on the selected formulation TG2. When the regression coefficient values of were compared, it was observed that ‘r’ values of first order was maximum i.e. 0.993 hence indicating drug release from formulations was found to follow Korsmeyer Peppas model release kinetics Conclusion: These results indicate that elastic liposome can function as probable drug delivery systems to enhance transdermal permeation of metronidazole for treating the topical infections. Keywords: Metronidazole, Elastic liposomes, Topical administration, Skin infection

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FORMULATION AND EVALUATION OF PERINDOPRIL MICROENCAPSULES BY USING DIFFERENT POLYMER

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i2.14899 ◽

2017 ◽

Vol 10 (2) ◽

pp. 153

Author(s):

Leena Jacob ◽

Abhilash Tv ◽

Shajan Abraham

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Release Rate ◽

Oral Drug Delivery ◽

Entrapment Efficiency ◽

Water Soluble ◽

Oral Drug ◽

Percentage Yield ◽

Drug Entrapment Efficiency

Objective: The study was carried out with an objective to achieve a potential sustained release oral drug delivery system of an antihypertensive drug, Perindopril which is a ACE inhibitor having half life of 2 hours. Perindopril is water soluble drug, so we can control or delay the release rate of drug by using release retarding polymers. This may also decrease the toxic side effects by preventing the high initial concentration in the blood.Method: Microcapsules were prepared by solvent evaporation technique using Eudragit L100 and Ethyl cellulose as a retarding agent to control the release rate and magnesium stearate as an inert dispersing carrier to decrease the interfacial tension between lipophilic and hydrophilic phase. Results: Prepared microcapsules were evaluated for the particle size, percentage yield, drug entrapment efficiency, flow property and in vitro drug release for 12 h. Results indicated that the percentage yield, mean particle size, drug entrapment efficiency and the micrometric properties of the microcapsules was influenced by various drug: polymer ratio. The release rate of microcapsules could be controlled as desired by adjusting the combination ratio of dispersing agents to retarding agents.Conclusion:Perindopril microcapsules can be successfully designed to develop sustained drug delivery, that reduces the dosing frequency and their by one can increase the patient compliance.

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Formulation and characterization of a paediatric nanoemulsion dosage form with modified oral drug delivery system for improved dissolution rate of nevirapine

MRS Advances ◽

10.1557/adv.2018.320 ◽

2018 ◽

Vol 3 (37) ◽

pp. 2203-2219 ◽

Cited By ~ 3

Author(s):

Tapiwa E. Manyarara ◽

Star Khoza ◽

Admire Dube ◽

Chiedza C. Maponga

Keyword(s):

Drug Release ◽

Dissolution Rate ◽

Oral Drug Delivery ◽

Cell Model ◽

Oral Drug ◽

Drug Efflux ◽

Inversion Point ◽

Improve Rate

ABSTRACTBackground: The development of appropriate dosage forms for paediatric antiretroviral therapy is key for improved therapeutic outcomes in children. The focus of this study was to improve solubility, dissolution rate, drug release and maintain high drug permeability.Methodology: A nanoemulsion was prepared using emulsion inversion point and evaluated. The nanoemulsion had nevirapine (3% w/w). In vitro drug release studies were performed using dialysis membrane. Permeability studies using the Caco-2 cell model were performed for the formulation.Results: The optimized nevirapine nanoemulsion had a mean droplet size of 36.09±12.27nm, low pdI of 0.598 and zeta potential of -7.87±4.35mV. At pH 2, the nanoemulsion released 76 ± 2 % of nevirapine within 2 h, while at pH 6.4 value representing the small intestine, amount of nevirapine released was 41.6± 4 %. The permeability rate of the nevirapine nanoemulsion was 30.02 x 10-6cm/s and higher than that of propranolol. Efflux ratio was 0.02 indicating low chance of drug efflux occurring.Conclusion: The results showed that a modified liquid drug release formulations of nevirapine could improve rate of dissolution and maintain high permeability and low drug efflux improving bioavailability of nevirapine in vivo.

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DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i3.23145 ◽

2018 ◽

Vol 11 (3) ◽

pp. 284

Author(s):

Pravin S Patil ◽

Shashikant C Dhawale

Keyword(s):

Particle Size ◽

Drug Release ◽

Dissolution Rate ◽

Drug Carrier ◽

Entrapment Efficiency ◽

Significant Rise ◽

Scanning Calorimetry ◽

In Vitro Drug Release

Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

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ENHANCEMENT OF DISSOLUTION CHARACTERISTICS OF CLOPIDOGREL BISULPHATE BY PRONIOSOMES

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i2.30575 ◽

2019 ◽

pp. 77-85 ◽

Cited By ~ 4

Author(s):

EMAN A. MAZYED ◽

SHERIN ZAKARIA

Keyword(s):

Drug Release ◽

In Vitro Release ◽

Entrapment Efficiency ◽

International Normalized Ratio ◽

Angle Of Repose ◽

Morphological Examination ◽

Span 60

Objective: The present investigation aims to formulate and evaluate proniosomes of clopidogrel bisulphate for improving its dissolution characteristics. Methods: The slurry method was used for the preparation of proniosomes of clopidogrel using cholesterol, sorbitan monostearate (Span 60) and maltodextrin as a carrier. Clopidogrel proniosomes were evaluated for their entrapment efficiency and in vitro drug release. The best formula (F1) that achieved maximum drug release was further evaluated by measurement of the angle of repose, morphological examination, determination of vesicle size, determination of zeta potential, Fourier transform infrared spectroscopy and differential thermal analysis. The in vivo behavior of the selected proniosomal formula (F1) was studied by measuring the antiplatelet activity in adult male mice. Results: The entrapment efficiency of clopidogrel proniosomes was in the range of 83.04±1.99 to 90.14±0.30. % drug released from proniosomal formulations was in the range of 79.73±0.35 to 97.70±1.10 % within 4 h. Clopidogrel proniosomes significantly enhanced the in vitro release of clopidogrel compared with the plain drug that achieved 61.77±2.22 % drug release. F1 significantly (p ≤ 0.001) increased the bleeding time and bleeding volume and significantly (p ≤ 0.05) prolonged prothrombin time and decreased prothrombin activity and increased the international normalized ratio (INR) compared to plain clopidogrel. Conclusion: The present investigation introduced proniosomes as a promising carrier for clopidogrel that could enhance its dissolution and pharmacological effect.

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