IMPROVEMENT OF THE DISSOLUTION PROFILE OF SIMVASTATIN TABLETS WITH THE ADDITION OF CREMOPHOR-EL USING WET GRANULATION METHOD

Objective: Simvastatin is a drug used as a first-line anti-cholesterol in the treatment of dyslipidemia. Low solubility will affect its ability to penetrate the digestive tract membrane and will affect the amount of drug levels in the plasma. The use of Cremophor-EL as a surfactant has been shown to inhibit the action of P-glycoprotein so that it can increase the bioavailability of a drug and can increase the effect of a drug. Methods: The preparation of simvastatin tablets was carried out using the wet granulation method. The dissolution test used the paddle method, a speed of 50 rpm at a temperature of 37±0.5 ° C with a phosphate buffer pH 7.0 as the dissolution medium. Results: The results showed that at 30 min the generic simvastatin tablets had 81.52% dissolution and the Simvastatin Tablets with Cremophor-EL were 85.520%. Conclusion: Simvastatin cremophor-EL tablets are more dissolved than generic simvastatin at 30 min so that cremophor-EL simvastatin tablets have a better dissolution rate than generic simvastatin tablets.

Mixed Pluronic—Cremophor Polymeric Micelles as Nanocarriers for Poorly Soluble Antibiotics—The Influence on the Antibacterial Activity

In this work, novel polymeric mixed micelles from Pluronic F127 and Cremophor EL were investigated as drug delivery systems for Norfloxacin as model antibiotic drug. The optimal molar ratio of surfactants was determined, in order to decrease critical micellar concentration (CMC) and prepare carriers with minimal surfactant concentrations. The particle size, zeta potential, and encapsulation efficiency were determined for both pure and mixed micelles with selected composition. In vitro release kinetics of Norfloxacin from micelles show that the composition of surfactant mixture generates tunable extended release. The mixed micelles exhibit good biocompatibility against normal fibroblasts MRC-5 cells, while some cytotoxicity was found in all micellar systems at high concentrations. The influence of the surfactant components in the carrier on the antibacterial properties of Norfloxacin was investigated. The drug loaded mixed micellar formulation exhibit good activity against clinical isolated strains, compared with the CLSI recommended standard strains (Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29213, Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922). P. aeruginosa 5399 clinical strain shows low sensitivity to Norfloxacin in all tested micelle systems. The results suggest that Cremophor EL-Pluronic F127 mixed micelles can be considered as novel controlled release delivery systems for hydrophobic antimicrobial drugs.

Formulation design and evaluation of aceclofenac nanogel for topical application

Aim: The current study aimed to explore the feasibility of the nanoemulgel for the topical delivery of aceclofenac. Materials & methods: Solubility of drugs in the formulation systems was determined and aceclofenac nanoemulsion (NE) was prepared by high-pressure homogenization technique. Carbopol 940 was added as a gelling agent. Results & conclusion: The composition of optimized NE consist of labrafil along with triacetin as oil, tween 80 and cremophor EL in combination as a surfactant and transcutol HP along with PEG 400 and ethanol as cosurfactant. The droplet size of the NE was 141.1 ± 3.65 nm, with low polydispersity index and negative zeta potential. The aceclofenac–nanoemulgel was developed using carbopol 940 and exhibited excellent permeation in comparison to the marketed sample.

Stability of Chlorophyll a Monomer Incorporated into Cremophor EL Nano-Micelles under Dark and Moderate Light Conditions

In this paper, stability of chlorophyll a monomers encapsulated into the Cremophor EL nano-micelles was studied under dark and moderate light conditions, typical of a room with natural or artificial lighting, in the presence of oxygen. The pigment stability against visible light was determined using the dynamic light scattering and molecular spectroscopy (UV-Vis absorption and stationary fluorescence) methods. Chlorophyll a, at the molar concentration of 10−5 M, was dissolved in the 5 wt% Cremophor emulsion for comparison in the ethanolic solution. The stability of such a self-assembly pigment–detergent nano-system is important in the light of its application on the commercial-scale. The presented results indicate the high stability of the pigment monomeric molecular organization in the nano-emulsion. During the storage in the dark, the half-lifetime was calculated as about 7 months. Additionally, based on the shape of absorption and fluorescence emission spectra, chlorophyll aggregation in the Cremophor EL aqueous solution along with the time was excluded. Moreover, the average size of detergent micelles as chlorophyll carriers was not affected after 70 days of the nano-system storage. Pigment stability against the moderate white light (0.1 mW) did not differ significantly from storage conditions in the dark. The photooxidation products, detected by occurrence of new absorption and fluorescence emission bands, was estimated on the negligible level. The stability of such a self-assembly pigment–detergent nano-system would potentially broaden the field of chlorophyll a (chl a) application in the food industry, medicine or artificial photosynthesis models.

Sodium 3-mercaptopropanesulphonate substituted phthalocyanine: Synthesis, photophysical properties, in vitro and in vivo PDT efficacy

A new sulfonic zinc(II) phthalocyanine bearing sodium 3-mercaptopropanesulphonate (Pc) was synthesized and characterized, as to its photophysical and photochemical properties, in vitro and in vivo. Pc remain non-aggregated in [Formula: see text],[Formula: see text]-dimethylformamide and in water containing 0.1% Cremophor EL, with high singlet oxygen efficacy. In vitro studies showed that the IC[Formula: see text] value of Pc on HepG2 cells was 1.3 [Formula: see text]M. In addition, in vivo studies showed that Pc mainly accumulated in tumor sites and showed an obvious PDT effect, and ca.97% of tumor growth was inhibited. Therefore, the Pc could be applied as a very promising photosensitizer for PDT in future clinical applications.

Topical Delivery of Coenzyme Q10-Loaded Microemulsion for Skin Regeneration

The aim of this study was to develop a coenzyme Q10 (CoQ10) microemulsion system with improved solubility, penetration, and wound healing efficacy. Based on the pseudo-ternary diagram, microemulsions containing isopropyl myristate (IPM), Cremophor EL®, and Transcutol® HP were selected and confirmed to be nanosized (<20 nm) and thermodynamically stable based on the dilution and thermodynamic stability tests. The CoQ10-loaded microemulsion with a surfactant/co-surfactant (S/CoS) ratio of 2:1 (w/w %) demonstrated a higher permeation efficacy compared to microemulsions with S/CoS ratio of 3:1 or 4:1 (w/w %). Additionally, the CoQ10-loaded microemulsion with an S/CoS ratio of 2:1 demonstrated a relatively rapid wound healing effect in keratinocytes and fibroblasts. Overall, these data suggest that a microemulsion based on IPM, Cremophor EL®, and Transcutol® HP could be an effective vehicle for the topical administration of CoQ10 and could be utilized for the application of other therapeutic agents that have difficulty in penetrating the skin.