Solid lipid nanoparticles are typically spherical with an average diameter between 1 and 1000 nm. It is an alternative carrier system to tradition colloidal carriers, such as, emulsions, liposomes, and polymeric micro and nanoparticles. Ramipril is an antihypertensive agent used in the treatment of hypertension. Its oral bioavailability is 28% and it is rapidly excreted through the renal route. This drug has many side effects such as, postural hypotension, hyperkalemia, and angioedema, when given as an immediate dosage form. To overcome the side effects and to increase the bioavailability of ramipril, solid lipid nanoparticles of ramipril are prepared by using lipids (glyceryl monostearate and glyceryl monooleate) with stabilizers (tween 80, poloxamer 188, and span 20). The prepared formulations have been evaluated for entrapment efficiency, drug content, in-vitro drug release, particle size analysis, scanning electron spectroscopy, Fourier transform-infrared studies, and stability. A formulation containing glyceryl monooleate, stabilized with span 20 as surfactant showed prolonged drug release, smaller particle size, and narrow particle size distribution, as compared to other formulations with different surfactants and lipids.
Solid lipid nanoparticles (SLNs) are an alternative carrier system used to load the drug for targeting, to improve the bioavailability by increasing its solubility, and protecting the drug from presystemic metabolism. The avoidance of presystemic metabolism is due to the nano-metric size range, so that the liver cannot uptake the drug from the delivery system and is not metabolized by the liver. Montelukast sodium is an anti-asthmatic drug, because of its poor oral bioavailability, presystemic metabolism, and decreased half-life; it was chosen to formulate as the solid lipid nanoparticle (SLN) system by hot homogenization followed by an ultrasonication method, to overcome the above. Compritol ATO 888, stearic acid, and glyceryl monostearate were used as a lipid matrix and polyvinyl alcohol as a surfactant. The prepared formulations have been evaluated for entrapment efficiency, drug content, in vitro drug release, particle size analysis, scanning electron microscopy, Fourier transform-infrared studies (FT-IR), differential scanning calorimetry (DSC), and stability. Particle size analysis revealed that the SLN prepared from the higher melting point lipid showed a larger particle size and with increased carbon chain length of the fatty acids. Entrapment efficiency (EE) was ranging from 42% to 92%. In vitro release studies showed maximum cumulative drug release was obtained for F 1 (59.1%) containing stearic acid, and the lowest was observed for F 18 (28.1%) containing compritol ATO 888 after 12 h and all the formulations followed first-order release kinetics. FT-IR and DSC studies revealed no interaction between drug and lipids. Studies showed that increase in lipid concentration, increased particle size, EE, and maintained the sustained release of drug. Among all, compritol ATO 888 was chosen as the best lipid for formulating SLN because it had high EE and sustained the drug release.
Psoriasis is a chronic condition that is caused by the negative signals given by immune system, which leads to hyperproliferation and other inflammatory reactions on the skin. These conditions may adversely affect the quality of the patient’s life leading to psychological stress. Topical delivery of drug is always preferred for Psoriasis because other treatments may lead to systemic intoxication and other adverse reactions. Triamcinolone is a topical corticosteroid belonging to BCS class IV (low solubility and permeability) used to treat Psoriasis. The limitations with transdermal delivery is that only a small amount of the drug can be transferred through the skin tissue due to the barrier effects of the Stratum corneum. Therefore, Novel transdermal delivery system, Cubosomes belonging to Nanostructured lipid carriers were chosen to overcome the issues of solubility and permeability. Twelve formulations were prepared with various ratios of Glyceryl monooleate (2.5 to 5%) & Poloxamer 407 (0.5 to 2%) and the formulations were evaluated for particle size, PDI, zeta potential, entrapment efficacy, drug content and in-vitro release. The best composition of Cubosomes was selected and incorporated into transdermal patch and the formulated patches were evaluated.
Hypertension is a chronic disease that is characterized by a persistently high blood pressure. It can cause strokes, myocardial infarctions, heart failure, and chronic kidney failure if not treated properly. An effort has been made to develop a fast dissolving tablet containing torsemide, which is used in the treatment of hypertension, in enhancing the onset of action, therapeutic response, patient acceptance, and ease of access. Torsemide fast dissolving tablets (FDTs) were prepared by direct compression method using different ratios of super-disintegrants. The prepared tablets were subjected to both pre and post evaluation parameters including Fourier Transform Infrared spectroscopy (FT-IR), Differential Scanning Calorimetry, Micromeritics properties, Hardness, weight variation, friability, disintegration time, wetting time, water absorption ratio and in-vitro dissolution studies. FTIR studies showed that the drug and excipients are compatible. According to the micromeritics analysis, all formulations had acceptable to good flow ability. Tablet hardness and friability indicated that the prepared formulations were having good mechanical strength. The formulation F27 which was prepared by using of super-disintegrant Crospovidone gave the good results for tablet disintegration, wetting time, and water absorption ratio and in-vitro dissolution.
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