Dissolution rate and stability study of flavanone aglycones, naringenin and hesperetin, by drug delivery systems based on polyvinylpyrrolidone (PVP) nanodispersions

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.

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Self-nanoemulsifying drug delivery systems (SNEDDS) and self-microemulsifying drug delivery systems (SMEDDS) as lipid nanocarriers for improving dissolution rate and bioavailability of poorly soluble drugs

Lipid Nanocarriers for Drug Targeting ◽

10.1016/b978-0-12-813687-4.00012-8 ◽

2018 ◽

pp. 473-508 ◽

Cited By ~ 7

Author(s):

Marko Krstić ◽

Đorđe Medarević ◽

Jelena Đuriš ◽

Svetlana Ibrić

Keyword(s):

Drug Delivery ◽

Dissolution Rate ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Poorly Soluble Drugs ◽

Lipid Nanocarriers ◽

Poorly Soluble

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Evaluation of Drug Dissolution Rate in Co-amorphous and Co-crystal Binary Drug Delivery Systems by Thermodynamic and Kinetic Methods

AAPS PharmSciTech ◽

10.1208/s12249-020-01864-0 ◽

2021 ◽

Vol 22 (1) ◽

Author(s):

Chunhui Hu ◽

Fabin Zhang ◽

Haining Fan

Keyword(s):

Drug Delivery ◽

Dissolution Rate ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Drug Dissolution ◽

Kinetic Methods

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Application of mixture experimental design in formulation and characterization of solid self-nanoemulsifying drug delivery systems containing carbamazepine

Hemijska industrija ◽

10.2298/hemind150623059k ◽

2016 ◽

Vol 70 (5) ◽

pp. 525-537 ◽

Cited By ~ 1

Author(s):

Marko Krstic ◽

Svetlana Ibric

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Dissolution Rate ◽

Droplet Size ◽

Drug Delivery Systems ◽

Polymorphic Form ◽

Delivery Systems ◽

Mixture Design ◽

Correlation Spectroscopy ◽

Solid Carrier

One of the problems with orally used drugs is their poor solubility, which can be overcame by creating solid self-nanoemulsifying drug delivery systems (SNEDDS). Aim is choosing appropriate SNEDDS using mixture design and adsorption of SNEDDS on a solid carrier to improve the dissolution rate of carbamazepine. Self-emulsifying drug delivery systems (SEDDS) consisting of oil phase (caprilic-capric triglycerides), a surfactant (Polisorbat 80 and Labrasol? (1:1)) and cosurfactant (Transcutol? HP) are formed by applying mixture design. 16 formulations were formulated, where proportion of lipids, surfactant and cosurfactant were varied (input parameters) in the following ranges: 10-30%, 40-60%, 30-50%, respectively. After dilution of SEDDS with water (90% water), the droplet size and polydispersity index (PdI) of the obtained emulsions (output parameters) were measured using photon correlation spectroscopy. After processing data, appropriate mathematical models that describe the dependence of input and output parameters were selected. The optimized SNEDDS was adsorbed on the carbamazepine and solid carrier physical mixture, containing 20% carbamazepine. Neusilin? UFl2, Neusilin? FL2, Sylysia? 320, diatomite were used as the carriers. The ratio of SNEDDS:carrier varied (1:1, 2:1). Dissolution testing was carried out in the rotation paddles apparatus. Caracterization of solid SNEDDS was performed using the hot stage microscopy (HSM), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), infrared spectrophotometry with Fourier transformation (FT-IR), scanning electron microscopy (SEM) and X-ray diffraction (PXRD). Selected SNEDDS consisting of lipids (21.12%), surfactant (42.24%) and cosurfactant (36.64%) had a droplet size 157.02?34.09 nm and PDI 0.184?0.021. Drug release profiles showed that in all formulations dissolution rate increased (the fastest drug release was observed in formulations with Sylysia? 320). It can be concluded that in all formulations carbamazepine is present in the thermodynamically most stable polymorphic form III. Formulation of solid SNEDDS can significantly increase dissolution rate carbamazepine, with conservation of the polymorphic form III CBZ and potentially increased bioavailability.

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Techniques For The Preparation of Tissue Samples Containing Injectable Polymer Microcapsules

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100120242 ◽

1985 ◽

Vol 43 ◽

pp. 710-711

Author(s):

G.E. Visscher ◽

R. L. Robison ◽

G. J. Argentieri

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Gastrocnemius Muscle ◽

Degradation Process ◽

Delivery Systems ◽

Tissue Reaction ◽

Electron Microscopic ◽

Tissue Samples ◽

Injectable Polymer ◽

Microscopic Techniques

The use of various bioerodable polymers as drug delivery systems has gained considerable interest in recent years. Among some of the shapes used as delivery systems are films, rods and microcapsules. The work presented here will deal with the techniques we have utilized for the analysis of the tissue reaction to and actual biodegradation of injectable microcapsules. This work has utilized light microscopic (LM), transmission (TEM) and scanning (SEM) electron microscopic techniques. The design of our studies has utilized methodology that would; 1. best characterize the actual degradation process without artifacts introduced by fixation procedures and 2. allow for reproducible results.In our studies, the gastrocnemius muscle of the rat was chosen as the injection site. Prior to the injection of microcapsules the skin above the sites was shaved and tattooed for later recognition and recovery. 1.0 cc syringes were loaded with the desired quantity of microcapsules and the vehicle (0.5% hydroxypropylmethycellulose) drawn up. The syringes were agitated to suspend the microcapsules in the injection vehicle.

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