8 research outputs found
Preparation and In Vitro/In Vivo Characterization of Porous Sublingual Tablets Containing Ternary Kneaded Solid System of Vinpocetine with β-Cyclodextrin and Hydroxy Acid
The demand for sublingual tablets has been growing during the previous decades especially for drugs with extensive hepatic first-pass metabolism. Vinpocetine, a widely used neurotropic agent, has low oral bioavailability due to its poor aqueous solubility and marked first-pass metabolism. Accordingly, the aim of this work was to develop tablets for the sublingual delivery of vinpocetine. Initially, the feasibility of improving vinpocetine’s poor aqueous solubility by preparing kneaded solid systems of the drug with β-Cyclodextrin and hydroxy acids (citric acid and tartaric acid) was assessed. The solid system with improved solubility and dissolution properties was incorporated into porous tablets that rapidly disintegrate permitting fast release of vinpocetine into the sublingual cavity. The pores were induced into these tablets by directly compressing the tablets’ excipients with a sublimable material, either camphor or menthol, which was eventually sublimated leaving pores. The obtained results demonstrated that the tablets prepared using camphor attained sufficient mechanical strength for practical use together with rapid disintegration and dissolution. In vivo absorption study performed in rabbits indicated that the sublingual administration of the proposed porous tablets containing vinpocetine solid system with β-Cyclodextrin and tartaric acid could be useful for therapeutic application
Cubosomes as Oral Drug Delivery Systems: A Promising Approach for Enhancing the Release of Clopidogrel Bisulphate in the Intestine
Nanoparticles as tool for enhanced ophthalmic delivery of vancomycin: a multidistrict-based microbiological study, solid lipid nanoparticles formulation and evaluation
Context: A microbiological multidistrict-based survey from different Egyptian governorates was conducted
to determine the most prevalent causative agents of ocular infections in the Egyptian population. Antibiotic
sensitivity testing was then performed to identify the most potent antimicrobial agent. Vancomycin (VCM) proved
the highest activity against gram-positive Staphylococcus bacteria, which are the most commonly isolated causative
agents of ocular infection. However, topically applied VCM suffers from poor ocular bioavailability because of its
high molecular weight and hydrophilicity. Objective: the aim of the present study was to develop VCM-loaded solid
lipid nanoparticles (SLNs) using water-in-oil-in-water (W/O/W) double emulsion, solvent evaporation technique to
enhance ocular penetration and prolong ophthalmic residence of VCM. Method: Two consecutive full factorial
designs (24
followed by 32
) were adopted to study the effect of different formulation and process parameters on SLN
formulation. The lipid type and structure, polyvinyl alcohol (PVA) molecular weight and concentration, sonication
time, as well as lipid:drug ratio were studied as independent variables. The formulated SLN formulae were
evaluated for encapsulation efficiency, particle size, and zeta potential as dependent variables. Results: The
statistically-optimized SLN formula (1:1 ratio of glyceryltripalmitate:vancomycin with 1% low molecular weight
PVA and 1 min sonication time) had average particle size of 277.25 nm, zeta potential of -20.45, and 19.99% drug
encapsulation. Scanning and transmission electron micrographs showed well-defined, spherical, homogenously
distributed particles. Conclusion: The present study suggests that VCM incorporation into SLNs is successfully
achievable; however, further studies with different nanoencapsulation materials and techniques would be valuable
for improving VCM encapsulation
Studying the influence of formulation and process variables on Vancomycin-loaded polymeric nanoparticles as potential carrier for enhanced ophthalmic delivery
Ocular topically applied Vancomycin (VCM) suffers poor bioavailability due to its high
molecular weight and hydrophilicity. In the Present investigation, VCM-loaded polymeric
nanoparticles (PNPs) were developed aiming to enhance its ocular bioavailability through
prolonging its release pattern and ophthalmic residence. PNPs were prepared utilizing double
emulsion (W/O/O), solvent evaporation technique. 2
3X4
1
full factorial design was applied to evaluate individual and combined influences of polymer type, Eudragit® RS100, sonication time,
and Span®
80 concentration on PNPs particle size, encapsulation efficiency, and zeta potential.
Further, the optimized formulae were incorporated in 1% Carbopol®
- based gel. In-vivo
evaluation of the optimized formulae was performed via Draize test followed by microbiological
susceptibility testing on albino rabbits. Results revealed successful formulation of VCM- loaded
PNPs was achieved with particle sizes reaching 155 nm and up to 88% encapsulation. Draize test
confirmed the optimized formulae as non-irritating and safe for ophthalmic administration.
Microbiological susceptibility testing confirmed prolonged residence, higher Cmax. with more
than two folds increment in the AUC(0.25- 24) of VCM-PNPs over control groups. Thus, VCMloaded
PNPs represent promising carriers with superior achievements for enhanced Vancomycin
ophthalmic delivery over the traditional use of commercially available VCM parenteral
powder after constitution into a solution by the ophthalmologists
Nanoparticles as tool for enhanced ophthalmic delivery of vancomycin: a multidistrict-based microbiological study, solid lipid nanoparticles formulation and evaluation
Microfinance as a tool for financing medical devices in Syria. An assessment of needs and a call for further research
Preparation and physicochemical characterization of dioctyl sodium sulfosuccinate (aerosol OT) microemulsion for oral drug delivery
The performance of dioctyl sodium sulfosuccinate (aerosol OT) in the development of a pharmaceutically acceptable, stable, self-emulsifying water continuous microemulsion with high dilution efficiency was assessed. A pseudoternary microemulsion system was constructed using aerosol OT/medium-chain triglycerides with oleic acid/glycerol monooleate and water. The model microemulsion was characterized with regard to its electroconductive behavior, eosin sodium absorption, interfacial tension, and droplet size measurements after dilution with water. The percolation transition law, which makes it possible to determine the percolation threshold and to identify bicontinuous structures, was applied to the system. The interfacial tension changes associated with the microemulsion formation revealed ultralow values up to 30% oil at a surfactant/cosurfactant ratio of 3∶1. Moreover, the investigated particle size and polydispersity using photon correlation spectroscopy after dilution with excess of the continuous phase proved the efficiency of the microemulsion system as a drug carrier that ensures an infinitely dilutable, homogeneous, and thermodynamically stable system