Drug localization and its effect on the physical stability of poloxamer 188-stabilized colloidal lipid emulsions

2021 ◽  
pp. 120394
Author(s):  
Nadine Francke ◽  
Heike Bunjes
Keyword(s):  
Physical Stability ◽  
Lipid Emulsions ◽  
Poloxamer 188 ◽  
Drug Localization

Polymeric Precipitation Inhibitor Based Supersaturable Self-microemulsifying Drug Delivery System of Canagliflozin: Optimization and Evaluation

2021 ◽  
Vol 18 ◽  
Author(s):  
Dilpreet Singh ◽  
Ashok K. Tiwary ◽  
Tejwant Singh Kang ◽  
Neena Bedi
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Physical Stability ◽  
In Vitro Dissolution ◽  
Titration Calorimetry ◽  
Substrate Affinity ◽  
Pharmacokinetic Studies ◽  
Poloxamer 188 ◽  
P Glycoprotein

Background: The present investigation attempts to optimize Supersaturable lipid based formulation (SS SMEDDS) of Biopharmaceutical Classification System (BCS) class IV drug canagliflozin (CFZ) and evaluating the oral bioavailability of the formulation. Methods: Preliminary screening revealed Poloxamer 188 to most effectively inhibit precipitation of CFZ after dispersion during in vitro supersaturation studies. Box Behnken Design was employed for designing different formulations and various statistical analysis were done out to select an appropriate mathematical model. The optimized formulation (OSS 1) was evaluated for in vitro drug release and ex vivo permeation studies to evaluate drug release and permeation rate. Pharmacokinetic studies have been done according to standard methodologies. Results: The optimized formulation (OSS 1) containing 781.1 mg SS SMEDDS and 2.24 % w/w Poloxamer 188 was developed at a temperature of 60°C which revealed nano-globule size with negligible aggregation. Isothermal titration calorimetry revealed the thermodynamic state of formed microemulsion with negative ∆G. The optimized formulation was observed to possess physical stability under different stress conditions and acceptable drug content.. In vitro dissolution of optimized SS SMEDDS revealed higher dissolution rate of CFZ as compared with native forms of CFZ. The permeability of CFZ from optimized SS SMEDDS across various excised segments of rat intestine was observed to be multifold higher that manifested in 2.05-fold higher Cmax and 5.64-fold higher AUC0-36h following oral administration to Wistar rats. Conclusion: The results could be attributed to substantial lymphatic uptake and P-glycoprotein substrate affinity of CFZ in SS SMEDDS investigated through chylomicron and P-glycoprotein inhibition approach, respectively.

Photostability Study on Character and Antioxidant Activity of Tomato Extract (Solanum lycopersicum l.) in Nanostructured Lipid Carrier (NLC) and Conventional Creame

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Noorma Rosita ◽  
Dewi Haryadi ◽  
Tristiana Erawati ◽  
Rossa Nanda ◽  
Widji Soeratri
Keyword(s):  
Antioxidant Activity ◽  
Physical Stability ◽  
Nanostructured Lipid Carrier ◽  
Uvb Radiation ◽  
K Value ◽  
Antioxidant Power ◽  
Solanum Lycopersicum L ◽  
Tomato Extract ◽  
Dpph Method ◽  
High Shear Homogenization

The aim of this study was to investigate the ability of NLC in increasing photostability of tomato extract in term of antioxidant activity. Photostability testing on antioxidant activity of samples were conducted by accelerating method using UVB radiation 32.400 joule for 21 hours radiation. Antioxidant activity was measured by DPPH method. NLC was made by High Shear Homogenization (HPH) method at 24000 rpm for 4 cycles, while conventional creame was made by low speed at 400 rpm. The product were characterized include: pH, viscosity, and particle size. There were had difference characters and physical stability. NLC had smaller size, more homogenous and more stable than conventional creame. It was known that stability of antioxidant activity of tomato extract in NLC system higher than in conventional creame. That was showed with k value, as constanta of rate scavenging activity decreasing in antioxidant power between time (Sigma 2-tail less than 0.005) of NLC and conventional creame were: 2.03x10-2 %/hour ±0.08 (3.94) and 4.71x 10-2 %/ hour ±0.23 (4.88) respectively.

Applications of Ion Exchange Resin in Oral Drug Delivery Systems

2017 ◽  
Vol 7 (03) ◽  
Author(s):  
Kathpalia Harsha ◽  
Das Sukanya
Keyword(s):  
Drug Delivery ◽  
Ion Exchange ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Physical Stability ◽  
Delivery Systems ◽  
Oral Drug ◽  
Ion Exchange Resins ◽  
Exchange Resins ◽  
Oral Drug Delivery Systems

Ion Exchange Resins (IER) are insoluble polymers having styrene divinylbenzene copolymer backbone that contain acidic or basic functional groups and have the ability to exchange counter ions with the surrounding aqueous solutions. From the past many years they have been widely used for purification and softening of water and in chromatographic columns, however recently their use in pharmaceutical industry has gained considerable importance. Due to the physical stability and inert nature of the resins, they can be used as a versatile vehicle to design several modified release dosage forms The ionizable drug is complexed with the resin owing to the property of ion exchange. This resin complex dissociatesin vivo to release the drug. Based on the dissociation strength of the drug from the drug resin complex, various release patterns can be achieved. Many formulation glitches can be circumvented using ion exchange resins such as bitter taste and deliquescence. These resins also aid in enhancing disintegrationand stability of formulation. This review focuses on different types of ion exchange resins, their preparation methods, chemistry, properties, incompatibilities and their application in various oral drug delivery systems as well as highlighting their use as therapeutic agents.

A Review on Microsponge Drug Delivery System

2020 ◽  
Vol 10 (2) ◽  
pp. 53-59
Author(s):  
Bharathi M ◽  
Mullaikodi O ◽  
Rajalingam D ◽  
Gnanasekar N ◽  
Kesavan M
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Physical Stability ◽  
Current Investigation ◽  
Considerable Time ◽  
Polymeric Structure ◽  
Point Of Interest ◽  
Time Period ◽  
Time Specific

A Microsponge (MS) is an extremely interconnected, permeable, polymeric structure that involves permeable microparticles trapping and discharging through the skin for a considerable time period. Drug delivery system (DDS) offer extended discharge with less degradation, improved physical stability along with better tolerance. The main intend of any DDS is to achieve the required amount of drug in plasma to produce the desired therapeutic and non-poisonous effect over a prolonged period of time. Specific methods for preparing MS were reviewed in this current investigation, and their pharmaceutical implementations were signed. MS have major DDS point of interest. It also improves stability, increased flexibility in formulation and increased elegance. In fact, numerous studies have reported that MS supplies are not allergic, mutagenic, and poisonous. MS creativity is used in products such as sunscreen, prescription, cosmetics, and OTC skin care. This inquiry primarily focuses on the different methods used to identify, plan and exploit MS.

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