Preparation and evaluation of lipid matrix microencapsulation for drug delivery of azilsartan kamedoxomil

The aim of the work is to consolidate azilsartan-kamedoxomil (AZM) into lipid matrix controlled-release microparticles to enhance its permeability because AZM belongs to Biopharmaceutical classification (BCS) IV which characterized by poor permeability and to protect AZM from light and humidity and execute a prolonged release profile. Materials and methods. A reversed-phase HPLC method was created and validated to estimate the drug. AZM microparticles formulations were invented using melt dispersion technique and waxy materials such as carnuba wax, beeswax, stearic acid in the ratio of waxy-substance: drug ranging from 0.25: 1 to 1:1 and stabilizer namely; tween 80 and Poloxamer 407 in ratio of stabilizer: drug ranging from 0.5:1 to 1:1. Azilsartan formulations were assessed for azilsartan-medoxomil content, loading, entrapment efficiency, the zeta potential,the particle size, the morphology by scanning electronic microscopy (SEM), and in-vitro release profile. Results. Zeta potential results for microparticle formulations using beeswax and carnuba range from -21.1 mV to -26.6 mV and -20.6 mV to -26.7 mV, respectively. This difference indicates that the azilsartan microparticles containing stearic acid are better stabilized with zeta potential of 25.3 - 29.7 mV. Furthermore, the release from azilsartan microparticle formulations containing stearic acid exceeded 80 % after 8 h and remained for 24 h while release from beeswax did not exceed 65 % after the same period and less than 60 % in case of carnuba formulations Conclusions. The formulation (AZSP4) exhibited the highest zeta potential and released exceeding 80 % of AZM over the course of 8 hours and remained over a day. AZSP4 microparticles formulation containing, poloxamer 407, in a 0.8:0.8:1 drug: stearic acid: poloxamer ratio proved the ability of stearic acid microencapsulation employing poloxamer as stabilizer in a certain ratio can prolong the release of AZ

Silybum marianum (Milk Thistle): Review on Its chemistry, morphology, ethno medical uses, phytochemistry and pharmacological activities

The oldest remedies identified to mankind are herbal medicines. India is recognized worldwide for its Ayurvedic treatment. India has rich history of using many plants for medicinal purposes. Remedial plants are cooperating extremely dynamic position in customary drugs for the action of a variety of illness. However a key obstacle, which has hindered the promotion in use of alternative medicines in the developed countries, is no evidence of documentation and absence of stringent quality control measures. There is a demand for the evidence of every investigate effort execute on conventional remedies in the appearance of certification. The purpose of current review is to make accessible up-to-date information on, botany, morphology, ecological biodiversity, therapeutic uses, phytochemistry and pharmacological activities on diverse parts of Silybum marianum (L.) Gaertn (S. marianum). This review was assembled using technical literature from electronic search engine such as Springer link, Bio Med Central, Pub Med, Scopus, Science Direct, Scielo, Medline and Science domain. Supplementary texts were obtained from books, book chapters, dissertations, websites and other scientific publications. S. marianum a member of the Asteraceae family, is a tall herb with large prickly white veined green leaves and a reddish-purple flower that ends in sharp spines. It is native of the Mediterranean region and which has also spread in East Asia, Europe, Australia and America. Confident chemical constituents were exposed cognate as silybin A, silybin B, isosilybin A, isosilybin B, silychristin, silydianin, apigenin 7-O-β-(2″- O-α-rhamnosyl)galacturonide, kaempferol 3-O-α-rhamnoside-7-O-β-galacturonide, apigenin 7-O-β-glucuronide, apigenin 7-O-β-glucoside, apigenin 7-O-β-galactoside, kaempferol-3-O-α-rhamnoside, kaempferol, taxifolin and quercetin. The plant is exclusively used as anti-diabetic, hepatoprotective, hypocholesterolaemic, anti-hypertensive, anti-inflammatory, anti-cancer, and as an anti-oxidant. Seeds of the plant are also used as an anti-spasmodic, neuroprotective, anti-viral, immunomodulant, cardioprotective, demulcent and anti-haemorrhagic. The plant is also serves as a galactagogue, agent that induces milk secretion and used in the treatment of uterine disorders. The plant is employed in dissimilar conventional schemes of remedy in the cure of different illness

Preparation and evaluation of lipid matrix microencapsulation for drug delivery of azilsartan kamedoxomil

The aim of the work is to consolidate azilsartan-kamedoxomil (AZM) into lipid matrix controlled-release microparticles to enhance its permeability because AZM belongs to Biopharmaceutical classification (BCS) IV which characterized by poor permeability and to protect AZM from light and humidity and execute a prolonged release profile. Materials and methods. A reversed-phase HPLC method was created and validated to estimate the drug. AZM microparticles formulations were invented using melt dispersion technique and waxy materials such as carnuba wax, beeswax, stearic acid in the ratio of waxy-substance: drug ranging from 0.25: 1 to 1:1 and stabilizer namely; tween 80 and Poloxamer 407 in ratio of stabilizer: drug ranging from 0.5:1 to 1:1. Azilsartan formulations were assessed for azilsartan-medoxomil content, loading, entrapment efficiency, the zeta potential,the particle size, the morphology by scanning electronic microscopy (SEM), and in-vitro release profile. Results. Zeta potential results for microparticle formulations using beeswax and carnuba range from -21.1 mV to -26.6 mV and -20.6 mV to -26.7 mV, respectively. This difference indicates that the azilsartan microparticles containing stearic acid are better stabilized with zeta potential of 25.3 - 29.7 mV. Furthermore, the release from azilsartan microparticle formulations containing stearic acid exceeded 80 % after 8 h and remained for 24 h while release from beeswax did not exceed 65 % after the same period and less than 60 % in case of carnuba formulations Conclusions. The formulation (AZSP4) exhibited the highest zeta potential and released exceeding 80 % of AZM over the course of 8 hours and remained over a day. AZSP4 microparticles formulation containing, poloxamer 407, in a 0.8:0.8:1 drug: stearic acid: poloxamer ratio proved the ability of stearic acid microencapsulation employing poloxamer as stabilizer in a certain ratio can prolong the release of AZ

Chitosan-decorated and tripolyphosphate-crosslinked pH-sensitive niosomal nanogels for Controlled release of fluoropyrimidine 5-fluorouracil

In the present study, 5-fluorouracil-loaded niosomal nanoparticles were successfully prepared and coated with chitosan and subsequently crosslinked by tripolyphosphate to form niosomal nanogels. The prepared niosomal formulations were fully characterized for their particle size, zeta potential, particle morphology, drug entrapment efficiency, and in vitro drug release profile. The prepared niosomal nanocarriers exhibited nanoscale particle sizes of 165.35 ± 2.75–322.85 ± 2.75 nm. Chitosan-coated and TPP-crosslinked niosomes exhibited a slightly decreased in particle size and a switch of zeta potential from negative to positive values. In addition, high yield percentage, drug encapsulation efficiency, and drug loading values of 92.11 ± 2.07 %, 66.59 ± 6.06, and 4.65 ± 0.5 were obtained for chitosan-coated formulations, respectively. Moreover, lowering the rate of 5-FU in vitro release was achieved within 72 h by using chitosan-coated formulations. All prepared formulations revealed hemocompatible properties in hemolysis assay with less than 5 % hemolysis percentage at their higher possible concentrations (500 µM and 1 mM). The cell viability by MTT assay showed higher anticancer activity against B16F10 cancerous cells and lower cytotoxicity toward NIH3T3 normal cells than control and pure 5-FU in the studied concentration range (10–100 µM). Investigating the cell migration inhibition properties of fabricated formulations revealed similar results with in vitro cell viability assay with a higher migration inhibition rate for B16F10 cells than NIH3T3 cells, controls, and free 5-FU