Optimum Entrapment Efficiency Research Articles

Smart perhydroxycucurbit [6] uril functionalized magnetic graphene oxide for release of Naringin as an antitumor agent

In this study, a mix ferrite (Zn0.6Co0.4Fe2O4) was immobilized on graphene oxide via a one pot hydrothermal method and the obtained magnetic nanocomposite was functionalized with a biocompatible, non-essential amino acid, glutamic acid, to provide functional sites. The final nanocomposite was obtained via conjugation of perhydroxycucurbit[6]uril which denoted as MFG-CB. The resulting compounds were characterized by transmission electron microscopy (TEM), field emission scanning electron microscopy (FE-SEM), energy dispersive X-ray spectroscopy (EDS), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), elemental analysis, vibrating sample magnetometry (VSM), the Brunauer– Emmet–Teller (BET) and zeta potential analysis. Concerning the model drug, Naringin was thereafter loaded onto the MFG-CB nanocomposite with an optimum entrapment efficiency (EE) of 98.73% and a loading capacity (LC) of 13.91%. The studies of in vitro release were conducted with regard to different pH and temperature conditions. Findings revealed the dependence of Naringin release from the nanocomposite on pH and temperature, with the maximum release achieved at pH = 5.4 at 45 °C. According to the model-dependent approach, the release mechanism was in line with the Korsmeyer-Peppas and first-order kinetic models. Finally, the in vitro cytotoxicity of the MFG-CB nanocomposite, Naringin-loaded MFG-CB was evaluated against human breast cancer (MCF-7) and human epithelial cervical cancer (HeLa) cell lines using N colorimetric assays. The results confirmed the improved cytotoxicity of Naringin by loading on the MFG-CB nanocomposite.

Development of Topical Antibacterial Gel Loaded with Cefadroxil Solid Lipid Nanoparticles: In vivo Wound Healing Activity and Epithelialization Study

Wound could be caused due to physical trauma or surgical incisions. The incidence of infection may extend the wound healing process. Thus, present study was aimed for the sustained drug release and site specificity in dermal region to eradicate the bacterial infection, thereby accelerate the wound healing process. Wound healing process was performed by the eradicating cutaneous infection with Cefadroxil loaded Solid Lipid Nanoparticles (SLN) based topical gels. Materials and Methods: Solid lipid nanoparticles of Cefadroxil (CEF) were prepared by solvent evaporation technique. Based on the particle and physicochemical characterizations one formulation was optimized. Selected formulation 1% w/w SLN4 was loaded in 1% w/v carbopol to develop topical antibacterial gel, which was evaluated for pH, spreadability, drug release and in vivo wound healing activity in male rats. Results: From the prepared five nanocarriers, SLN4 was selected that showed nanorange size, stable, monodispersed particles, with the optimum entrapment efficiency and drug loading. Fourier-transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and X-Ray Diffraction (XRD) presented that CEF was encapsulated and available in the non-crystalline form in SLN. Polymeric gel loaded with CEF-SLN4 has desired pH and spreadability with 86.76 +/- 0.12% of drug released in 8 h. Whereas in vivo wound healing activity was assessed as wound contraction and noted to be 99.73 +/- 0.93% within 3 weeks alongside complete epithelialization was achieved within 17 days by the application of CEF-SLN4 gel. Conclusion: Prepared CEF-SLN4 gel was stable, skin-compatible and spreadable with sustained drug release. Applied gel efficiently permeable deeper into skin layers, eradicate the bacterial growth and could be effective in treating the infectious wound in short-span of time. Therefore, CEF-SLN4 topical gel could be efficiently used for the faster wound healing treatment.

Evaluations of Quality by Design (QbD) Elements Impact for Developing Niosomes as a Promising Topical Drug Delivery Platform.

Topical corticosteroids are used to treat a variety of skin conditions such as allergic reactions, eczema, and psoriasis. Niosomes are a novel surfactant-based delivery system that may be used to deliver desoximetasone via topical product application in order to mitigate common side effects associated with traditional oral delivery routes. The aim of this research was to identify the critical material attributes (CMAs) and critical process parameters (CPPs) that impact key characteristics of drug-loaded niosomes using a systematic quality by design (QbD) approach. An organic phase injection method was developed and used to manufacture the niosomes. The CMAs were identified to be drug amount, concentrations of surfactant and cholesterol, and types of lipids. The CPPs were phase volumes, temperature, mixing parameters, and addition rate based on previous research. The quality attributes measured were entrapment efficiency, particle size distribution, PDI, and zeta potential. These were used to determine the quality target product profile (QTPP) of niosomes. The experimental data indicate that the critical impacting variables for niosomes are: surfactant and cholesterol concentrations, mixing parameters, and organic-phase addition rate. Based on the experimental results of this study methanol:diethyl ether (75:25) as the organic system, drug:surfactant:cholesterol in 1:2:1 concentration, stearic acid as the charge-inducing material, 20 mL external phase and 10 mL internal phase volume, 65 °C external phase temperature, 60 min mixing time, 650 RPM mixing speed and 1 mL/ml addition rate is the ideal combination to achieve desirable desoximetasone niosomes with optimum entrapment efficiency and particle size for topical application.

FORMULATION EVALUATION AND OPTIMIZATION OF CHITOSAN COATED CEFTRIAXONE LOADED MICROPARTICLES

Ceftriaxone, a third generation cephalosporin antibiotic is an important antibiotic used in the treatment of invasive infections caused by the certain bacteria such as the penicillin-resistant microorganisms like Staphyloccocus aureus, strains of S. pneumonia, S. aureus and Enterobacteriaceae , particularly among E. coli. There is increasing antimicrobial resistance of Ceftriaxone in particular against these strains of bacteria. This study has been conducted to formulate, evaluate and optimize chitosan coated ceftriaxone loaded microparticles with better efficacy and also observes the MIC against strains of bacteria. Emulsion crosslinking method was used for the formulation of microparticles of ceftriaxone by using chitosan as a polymer and glutraldehyde as a cross linking agent which is optimized by using Box-Behnken Design. Three independent variables were taken; effect of drug and the polymer ratio, effect of the stirring speed and effect of crosslinking agent and dependent variables were microparticles entrapment efficiency and the In vitro drug release. Following optimization of the formulations, physical characterization as well as entrapment efficiency and ultimately in-vitro evaluation was performed. Physical characterization include optical microscopy, SEM and DLS to check there physical properties. The method used for the formulation of microparticle had the optimum entrapment efficiency of 61.7% which was increase with the increase in the addition of the more amount of chitosan and glutraldehyde and method also achieved the good in vitro release. MIC studies of microparticles were done against Klebsiella pneumonia, Staphylococcus aureus, Streptococcus mutans, Escherichia coli and it was found that the formulations showed decrease in MIC.

Improving the in vitro penetration of niacinamide using span 60-based niosomal system in gel formulation

Niacinamide is one of the components of cosmeceutical products that reported to have skin benefits for the treatment of skin pigmentation, acne and wrinkles. However, the dermal penetration of niacinamide is poor. The carrier system which can be selected to carry the compound through the stratum corneum layer is the niosome system using span 60. This study was aimed to determine the concentration of span 60 that can trap niacinamide optimally and the ability of niosome system span 60 to increase in vitro penetration of niacinamide in gel formulation. The different formulations of nicotinamide niosome were formulated with variance concentrations of Span 60, that is, formula A 100 μmol, formula B 150 μmol, and formula C 200 μmol. The entrapment efficiency testing was conducted using dialysis membrane. The gel formulation was prepared in two formulas, niacinamide niosome gel and niacinamide gel (without niosomes) and tested diffusion using Franz diffusion cell flow-through type. The result show that Formula A provides the most optimum entrapment efficiency of 99.03±0.026%. The results of the in vitro skin penetration studies for 8 hours indicate that the niosomal formulation using Span 60 could increase skin penetration with the percent cumulative amount of niacinamide niosomes was 82.87±1.6932% compared to niacinamide in gel without noisome system about 70.27±5,3212%.

Nanostructured lipid carriers of olmesartan medoxomil with enhanced oral bioavailability

The current study explores the potential of nanostructured lipid carriers (NLCs) for oral bioavailability enhancement of olmesartan medoxomil (OLM) by systemic design approach. OLM-NLC was successfully prepared with optimized process parameters (i.e. amount of liquid lipid, total amount of lipid, drug content and surfactant concentration) using the Box-Behnken design of experiments for different response parameters (i.e. particle size, Polydispersity index and entrapment efficiency). Further, optimized formulation was validated which depicted nano size, homogenous distribution with optimum entrapment efficiency. OLM-NLC was characterized by different techniques viz. differential scanning calorimetry (DSC), powder X-Ray diffraction (PXRD), scanning electron microscopy (SEM) and transmission electron microscopy (TEM), which showed reduced crystallinity of the drug with smooth spherical appearance of nanoparticles. Formulation was found to be stable in simulated gastric fluids as no significant changes were found in size, PDI and entrapment efficiency. In vitro release showed extended release of OLM from OLM-NLC. In vitro cellular uptake study revealed 5.2 folds higher uptake of nanoparticles as compare to the free drug, when incubated with Caco-2 cells. In vivo performance showed that AUCtotal and Cmax of OLM-NLC were found significantly (P<0.01) higher as compare to the free drug. Overall, the present study successfully reports the improvement of oral bioavailability of olmesartan medoxomil.

Modeling, Optimization, and In Vitro Corneal Permeation of Chitosan-Lomefloxacin HCl Nanosuspension Intended for Ophthalmic Delivery

Lomefloxacin HCl (LF) is a widely used fourth-generation fluoroquinolone antibiotic. Like most drug solutions administered via ocular route, it is usually eliminated by eye protective mechanisms. Chitosan (CS) is a natural polysaccharide polymer with numerous advantages in ocular delivery with, antibacterial, and antifungal properties. The aims were to formulate and optimize LF nanosuspensions (NS) with enhanced antimicrobial activity and prolonged duration using ionic gelation technique. Formulation variables included drug load, CS concentration, crosslinker type (tripolyphosphate and sodium alginate), and concentration. Nanosuspension properties (particle size, zeta potential, polydispersity index, entrapment efficiency, drug release, and permeation through bovine cornea) were evaluated. The artificial neural networks (ANNs) model showed optimum entrapment efficiency of 70.63 % w/w, particle size of 176 ± 0.28 nm, and zeta potential of 13.65 mV. Transmission electron microscopy illustrated the production of well-defined spherical nanoparticles. The nanosuspensions showed prolonged release of LF for more than 8 h and threefold increase in amount permeated through bovine cornea compared to drug solution. Improved antibacterial activity of the nanosuspension was noted where 2- and 3.5-fold decrease in minimum inhibitory concentration (MIC) of drug against Gram-positive and Gram-negative bacteria were observed, respectively. Twofold decrease in minimum bactericidal concentration (MBC) of drug nanosuspension against both types of bacteria was also demonstrated. Histopathological examination showed compatibility of optimized formulation with eye tissues in rabbit model. Therefore, model-optimized LF nanosuspension could be an ideal solution to ocular infections by virtue of their augmented activity, high compatibility, and improved permeability.

Formulasi Mikrokapsul Ranitidin HCl Menggunakan Rancangan Faktorial dengan Penyalut Etil Selulosa

Ranitidin HCl adalah H2-antagonis histamin yang digunakan dalam pengobatan ulkus lambung dan duodenum. Formulasi mikrokapsul ranitiditin HCl ditujukan untuk memperpanjang regimen dosis untuk meningkatkan bioavailabilitas dan waktu paruh. Tujuan dari penelitian untuk merumuskan dan mengoptimalkan mikrokapsul ranitidin HCl untuk menyiapkan sistem pelepasan yang sesuai dengan desain faktorial. Mikrokapsul disusun menggunakan etilselulosa dengan teknik penguapan pelarut. Variasi konsentrasi penstabil Span 80 (1-2%) dan rasio obat/polimer (2: 2-1: 2) dilakukan untuk mengamati efek efisiensi penjerapan. Analisis data menunjukkan bahwa mikrokapsul dengan efisiensi penjerapan optimal didapatkan pada formula yang mengandung 2% span 80, dan 1:2 rasio obat/polimer. Hasil penelitian menunjukkan mikrokapsul berbentuk sferis, dan berpori, dengan waktu pelepasan hingga 10,55 jam.

Development and Evaluation of Chitosan Based Polymeric Nanoparticles of an Antiulcer Drug Lansoprazole

Article history: Objective: The development of new delivery systems for the controlled release of drugs is one of the most innovative fields of research in pharmaceutical sciences. Nanoparticles specially designed to release the drug in the vicinity of target sites. The aim of this study was to formulate and evaluate the Lansoprazole nanoparticles to improve the therapeutic efficacy of Lansoprazole by loading in nanoparticle drug delivery system. Materials and Methods: Lansoprazole loaded chitosan nanoparticles (CNP1 to CNP10) were prepared by ionotropic gelation method. The formulated nanoparticles were evaluated for external morphological characters, determination of particle size analysis, zeta potential, drug content, entrapment efficiency and in-vitro release studies. Results: The drug content for the Lansoprazole loaded chitosan nanoparticles varied from 69.5±7.2% to 87.9±1.2%. The entrapment efficiencies were found to be minimum and maximum of 39.3±2.6% and 85.6±1.2%, the optimum entrapment efficiency was found to be 85.3±0.8%, particle size varied from 360±12nm to 814±62nm, zeta potential values were in positive and increased from 11.2±1.2mV to 18.7±0.4mV. In-vitro release of drug follows zero order and showed sustained release behavior for a period of 24 hr. Conclusion: The study demonstrated the successful preparation of sustained release polymeric nanoparticles of Lansoprazole.

Surface structured liposomes for site specific delivery of an antiviral agent-indinavir

The present investigation was aimed at targeting indinavir, a protease inhibitor to cells of mononuclear phagocyte system (MPS) via mannosylated liposomes. β-d-1-thiomannopyranoside residues were covalently coupled with dimyristoyl phosphatidylethanolamine (DMPE) to generate mannosylated-DMPE (Man-DMPE) conjugate which was further incorporated with disteroyl phosphatidyl choline and cholesterol to prepare mannosylated liposomes. The optimized mannosylated liposomes were nanometric in size (142 ± 2.8 nm) with optimum entrapment efficiency (88.7 ± 2.3%). Less than 20% cumulative drug release was observed from the prepared formulations in 24 h in phosphate buffer saline (pH 7.4). Cellular uptake studies performed on J774.A1 macrophage cell line via flow cytometric analysis depicted enhanced uptake of mannosylated liposomes as compared to plain liposomes. Annexin-V-fluorescein isothiocyanate/propidium iodide apoptosis assay delineated marginal cytotoxicity in macrophages from the developed formulation. Plasma and tissue distribution studies performed to assess the drug reach to macrophage rich regions depicted a significant level (P < 0.05) of indinavir in macrophage rich tissues like liver, spleen, and lungs from mannosylated liposomes as compared to plain liposomes and free drug. The conducted studies suggest the potential of indinavir loaded mannosylated liposomes for anti-human immunodeficiency virus therapy.