scholarly journals FORMULATION AND EVALUATION OF SUBMICRON EMULSION CONTAINING ENTRAPPED FLUOROQUINOLONE FOR OCULAR DELIVERY

2018 ◽  
Vol 11 (7) ◽  
pp. 431 ◽  
Author(s):  
Durga Pandey ◽  
Deepti Jain
Keyword(s):  
Drug Release ◽  
Penetrating Trauma ◽  
Spherical Shape ◽  
High Energy ◽  
In Vitro Drug Release ◽  
Transmission Electron ◽  
Sustain Release ◽  
Submicron Emulsion

Objective: The objective of the present work was to develop and characterize the submicron emulsion bearing antimicrobial drug sparfloxacin for improvement of ocular activity by improved retention in eyes. The developed delivery system was results with prolonged drug release as compared to the conventional dosage form.Methods: SE prepared by high energy emulsification and sonication to obtain uniform globule size.Results: Average internal droplets size of the optimized formulation was 0.278±0.6 μm, pH of the optimized formulation was 6.9±0.6 (average of three determinations), and viscosity 2.9±0.5 cps suitable for ocular use. Entrapment of SF was 63±3.4%. Stable under accelerated and long-term at 4°C and 37°C. No major changes reported on pH and viscosity of optimized formulations. In vitro, drug release pattern showed sustain release of SF, a cumulative percent release of SF was found 87.8±1.7% within 24 h. Transmission electron microscopy showed spherical shape and size within 1 μm.Conclusion: Designed formulation can be a good candidate for ocular drug delivery for severe ocular infections where frequent dosing required for conditions such as endophthalmitis, corneal ulcer, and penetrating trauma. 

scholarly journals IMPROVED CIPROFLOXACIN PENETRATION IN GOAT EYES USING COMPLEXATION TECHNIQUE

2019 ◽  
pp. 168-171
Author(s):  
DURGA PANDEY ◽  
DEEPTI JAIN
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Penetrating Trauma ◽  
Spherical Shape ◽  
High Energy ◽  
Ion Pair ◽  
Precipitation Method ◽  
Globule Size ◽  
Sustain Release

Objective: The objective of the present work was to improve the retention and penetration of ciprofloxacin (CF) ion pair entrapped within submicron emulsion (SE) in goat eyes and characterize the SE for improvement of ocular activity. The developed delivery system resulted with prolonged drug release as compared to the conventional dosage form. Methods: SE prepared by high-energy emulsification and sonication to obtain uniform globule size. Ion-pair complex is prepared by precipitation method. Results: Average internal droplets size of the optimized formulation was 0.300 μm, pH of the optimized formulation was 6.4±0.7 (average of three determinations) and viscosity 3.2±0.3 cP suitable for ocular use. Entrapment was 92.12%. In vitro drug release pattern in dialysis membrane showed sustain release of CF, a cumulative percent release of CF was found 77% in 10 h. Scanning electron microscopy showed spherical shape and size within 1 μm. In vitro release in goat eyes was found 35.86 % for optimized formulation compared to market, 26.83% in 60 min. Conclusion: Developed optimized formulation can be a good candidate for ocular drug delivery in severe ocular infections where frequent dosing required such as endophthalmitis, corneal ulcer, and penetrating trauma.

scholarly journals Novel Contact Lenses Embedded with Drug-Loaded Zwitterionic Nanogels for Extended Ophthalmic Drug Delivery

Nanomaterials ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 2328
Author(s):  
Zhao Wang ◽  
Xinhua Li ◽  
Xiaojuan Zhang ◽  
Ruilong Sheng ◽  
Qing Lin ◽  
...  
Keyword(s):  
Drug Release ◽  
Contact Lenses ◽  
Eye Drops ◽  
Water Contact ◽  
In Vitro Drug Release ◽  
Molding Method ◽  
Ophthalmic Drug ◽  
One Step

Therapeutic ophthalmic contact lenses with prolonged drug release and improved bioavailability have been developed to circumvent tedious eye drop instillation. In this work, zwitterionic nanogels based on poly(sulfobetaine methacrylate) (PSBMA) were easily fabricated by one-step reflux-precipitation polymerization, with the advantages of being surfactant-free and morphology controlled. Then, the ophthalmic drug levofloxacin (LEV) was encapsulated into the nanogels. A set of contact lenses with varied nanogel-loading content was fabricated by the cast molding method, with the drug-loaded nanogels dispersed in pre-monomer solutions composed of 2-hydroxyethyl methacrylate (HEMA) and N-vinyl-2-pyrrolidone (NVP). The structure, surface morphology, water contact angle (WCA), equilibrium water content (EWC), transmittance, and mechanical properties of the contact lenses were subsequently investigated, and in vitro drug release and biocompatibility were further evaluated. As a result, the optimized contact lens with nanogel-loading content of 8 wt% could sustainably deliver LEV for ten days, with critical lens properties within the range of recommended values for commercial contact lenses. Moreover, cell viability assays revealed that the prepared contact lenses were cytocompatible, suggesting their significant potential as an alternative to traditional eye drops or ointment formulations for long-term oculopathy treatment.

scholarly journals DESIGN AND EVALUATION OF SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEMS OF ALVERINE FOR ENHANCEMENT OF SOLUBILITY

2021 ◽  
Vol 12 (7) ◽  
pp. 25-31
Author(s):  
Pooja . ◽  
Pankaj Kumar Sharma ◽  
Viswanath Agrahari
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Ethyl Oleate ◽  
Spherical Shape ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Transmission Electron ◽  
The Stability

Background: The aim of this study is to develop a liquid self-nano emulsifying drug delivery system for alverine (liquid-SNEDDS).Excipients in the alverine SNEDDS include Ethyl oleate as the oil phase, Tween 80 as a surfactant, and PEG600, Propylene glycol as a cosurfactant.The prepared eleven formulations of alverine SNEDDS were performed for emulsification time, percentage transmittance, particle size, drug release, in vitro dissolution and stability studies.The optimised alverine liquid SNEDDS formulation (D1) was studied for drug-excipient compatibility using infrared spectroscopy, as well as particle size, zeta potential, transmission electron microscopy, and stability. Alverine SNEDDS have a spherical shape with uniform particle distribution, according to their morphology. D1's optimised formulation's drug release percentage (96.6). The stability data revealed no discernible changes in drug content, emulsifying properties, drug release, or appearance. As a result, a potential SNEDDS formulation of alverine with improved solubility, dissolution rate, and bioavailability was developed.

scholarly journals INFLUENCE OF BIOENHANCERS ON THE RELEASE PATTERN OF NIOSOMES CONTAINING METHOTREXATE

2012 ◽  
Vol 02 (02) ◽  
pp. 36-40
Author(s):  
Narayana Charyulu R. ◽  
Gandhi Kinjal B. ◽  
Jobin Jose ◽  
Sneh Priya ◽  
Shastry C. S.
Keyword(s):  
Thin Film ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Pattern ◽  
Sustain Release ◽  
Pure Drug ◽  
Span 60 ◽  
Dicetyl Phosphate

AbstractThe aim of present study was to prepare sustained release formulations of niosomes of methotrexate (MTX) alone (N1 to N10) and along withbioenhancers (NB1 to NB9) by thin film hydration technique using span 60 as surfactant,cholesterol as membrane stabilizing agent, curcumin and piperine as bioenhancers and dicetyl phosphate (DCP) as charge inducing agent. All the formulations of niosomeswere characterized on the basis of physical appearance and entrapment efficiency. The invitro releasestudies of optimized formulation of niosomes of MTX alone and along with bioenhancers were performed and compared with pure drug released. The entrapment efficiency of MTX in optimized formulation of niosomes containing MTX along with bioenhancers was found to 56.9% and entrapment efficiency of bioenhancerscurcumin and piperinewas found to be 40.30% and 69.1%respectively. In vitro drug release of optimized formulationsof niosomes of MTX without and with bioenhancers (F3) was found to be 98.89% and 60.97% at the end of 12 h respectively. Results concluded that Niosomes of MTX containing bioenhancers followed sustain release pattern.

scholarly journals Formulation and evaluation of floating microspheres of losartan potassium using sodium alginate and HPMC by solvent evaporation method

2019 ◽  
Vol 9 (1-s) ◽  
pp. 60-66 ◽  
Author(s):  
Kapil Purohit ◽  
Navneet Garud
Keyword(s):  
Drug Release ◽  
Solvent Evaporation ◽  
Losartan Potassium ◽  
Solvent Evaporation Method ◽  
In Vitro Drug Release ◽  
Evaporation Method ◽  
Sustained Action ◽  
Improve Patient

Hollow multі-unіt mіcrospheres were prepared by a solvent dіffusіon technіque іn emulsіon wіth a drug and an acrylіc polymer. These were dіssolved іn a mіxture of ethanol-dіchloromethane and poured іnto an aqueous solutіon of PVA wіth stіrrіng to form emulsіon droplets. The rate of drug release іn mіcro balloons was controlled by changіng the ratіo of polymer to drug. The mіcroballoons were floatіng іn vіtro for 12-24 hours when submerged іn aqueous medіa. Radіographіc studіes showed that mіcroballons admіnіstered orally to humans were dіspersed іn the upper part of the stomach and were held there for 3 hours agaіnst perіstaltіc movement. Floating Microspheres of Losartan potassium were formed by Solvent Evaporation method .The formulas LP7 of Losartan Potassium Floating Microspheres shows a very good drug release profiles and shown better sustained action till the end of last hour (24th hrs). It will improve patient compliance and increase in bioavailability which give better approach to treat hypertensive condition and the angiotensin receptor blocking action of Losartan lower the long term complications of Hypertension and reduce the risk of heart failure, CHF, Myocardial Infarction and also vascular damage in blood vessels and kidney. Keywords: Losartan Potassium, Floating microspheres, Drug Entrapment, In-vitro drug release.

Preparation of ciprofloxacin-encapsulated poly-ε- caprolactone microcapsules by the solvent evaporation technique

e-Polymers ◽  
2013 ◽  
Vol 13 (1) ◽  
Author(s):  
Marta Przybyslawska ◽  
Aleksandra Amelian ◽  
Katarzyna Winnicka
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
Evaporation Technique

Abstract The objective of this study was to prepare ciprofloxacin (CIP) encapsulated poly-ε-caprolactone (PCL) microcapsules by the single emulsion oilin- water (o/w) solvent evaporation method. The obtained microcapsules were characterized for size, morphology, drug loading and entrapment efficiency. The physical state of microcapsules was determined by differential scanning calorimetry (DSC) and thermogravimetric analysis (TG). Storage stability, the in vitro drug release and mathematical modeling of drug release were also tested. It was found that obtained microcapsules had spherical shape and their size range was from 57.5 μm to 234.7 μm. The drug loading of microcapsules was from 1.72% to 11.02%. The optimal conditions of the encapsulation process include the drug/polymer ratio 2/1, using homogenizer for 5 min at 15000 rpm to disperse CIP in PCL solution and aqueous phase at pH 5.5. The results of CIP release study indicate that obtained microcapsules might be successfully used for designing sustained release dosage forms.

scholarly journals Development of local strontium ranelate delivery systems and long term in vitro drug release studies in osteogenic medium

2018 ◽  
Vol 8 (1) ◽  
Author(s):  
Dagnija Loca ◽  
Anastasija Smirnova ◽  
Janis Locs ◽  
Arita Dubnika ◽  
Jana Vecstaudza ◽  
...  
Keyword(s):  
Drug Release ◽  
Strontium Ranelate ◽  
Delivery Systems ◽  
Osteogenic Medium ◽  
In Vitro Drug Release ◽  
Release Studies

scholarly journals Recent Progress in Drug Release Testing Methods of Biopolymeric Particulate System

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1313
Author(s):  
Yejin Kim ◽  
Eun Ji Park ◽  
Tae Wan Kim ◽  
Dong Hee Na
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Testing Methods ◽  
In Vitro Drug Release ◽  
Particulate System ◽  
Vitro Release ◽  
Release Testing

Biopolymeric microparticles have been widely used for long-term release formulations of short half-life chemicals or synthetic peptides. Characterization of the drug release from microparticles is important to ensure product quality and desired pharmacological effect. However, there is no official method for long-term release parenteral dosage forms. Much work has been done to develop methods for in vitro drug release testing, generally grouped into three major categories: sample and separate, dialysis membrane, and continuous flow (flow-through cell) methods. In vitro drug release testing also plays an important role in providing insight into the in vivo performance of a product. In vitro release test with in vivo relevance can reduce the cost of conducting in vivo studies and accelerate drug product development. Therefore, investigation of the in vitro–in vivo correlation (IVIVC) is increasingly becoming an essential part of particulate formulation development. This review summarizes the principles of the in vitro release testing methods of biopolymeric particulate system with the recent research articles and discusses their characteristics including IVIVC, accelerated release testing methods, and stability of encapsulated drugs.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

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