Modified Solvent Diffusion Method Research Articles

Design, Development and Optimization of Solid Lipid Nanoparticles of Rizatriptan for Intranasal delivery: Invitro & Invivo assessment

Solid lipid nanoparticles were at the frontline of the rapid development of nanotechnology, with several potential applications in drug administration. Because of their unique size-dependent properties, solid lipid nanoparticles have the potential to produce innovative treatments. The capacity to incorporate drugs into nanocarriers allows for the creation of a revolutionary drug delivery prototype that might be utilized for targeting novel drugs to the brain. RZT benzoate intra nasal formulation would be a practical, non-invasive, & alternative method of fast drug delivery to the brain for migraine treatment. Poloxamer-containing solid lipid nanoparticles having mucoadhesive characteristics improve drug absorption by increasing contact duration at the nasal mucosa. Shape, surface morphology, particle size, FTIR, DSC, X-ray diffraction tests, drug entrapment, total drug content, and in vitro drug release studies were all performed on RZT-loaded solid lipid nanoparticles created utilizing a modified solvent diffusion method. There was a wide range in particle size from 124.9 to 467.2 nm for these lipid nanoparticles, all of which were spherical and smooth on the outside. There was a maximum in vitro drug release of 92.6% in 24 h, a drug content of 45–55%, and a maximum entrapment efficacy of 78.6 percent. When administered through the nose, RZT benzoate may be more bioavailable than when taken orally, overcoming the first-pass impact and allowing for a long-term therapy plan for acute migraine.

Smart PLGA nanoparticles loaded with Quercetin: Cellular uptake and in-vitro anticancer study

Flavonoids have gained attention in cancer chemotherapy due to promising pre-clinical results. Flavonoids are constrained in therapeutics for solubility and permeability limitations. Quercetin (Qr) is a most abundant flavonoid in plants. Smart nanoparticle drug delivery devices were designed for better delivery of Qr. Transferrin was used for nanoparticle ligand tethering for successful particle propagation up to the cancer cell nucleus. PLGA nanoparticles loaded with Qr (QrPLGA) were prepared in modified solvent diffusion method using pluronic as a stabilizer. Transferrin conjugation on QrPLGA (Tf-QrPLGA) was achieved in EDC/NHS coupling reactions. Nanoparticles were characterized in DLS, AFM, TEM and FTIR. In-vitro anticancer efficacy was evaluated in metastatic cancer cell lines. The average particle size in DLS was 150 nm. The entrapment efficiency of Qr (70.52%) and non-fickian release pattern were observed by RP-HPLC. The FTIR analysis confirmed Tf interactions with nanoparticles. Tf-QrPLGA showed significantly strong antiproliferative and cytotoxic effects on both the cancer cell lines. Time-dependent uptake and quantitative count in flow-cytometry showed early time-point intracellular entry of Tf-QrPLGA. Specific cellular localization was confirmed by confocal microscopy. Increased sub-G1 population and decreased G2/M population demonstrating the apoptotic potential and cellular arrest of Tf-QrPLGA on cancer cells.

Development and optimization of ifosfamide nanostructured lipid carriers for oral delivery using response surface methodology

The research focuses on the development and optimization of ifosfamide nanostructured lipid carriers for oral delivery with the application of response surface methodology. The objectives of the study were to develop a formulation for ifosfamide to be delivered orally, overcome the instability of the drug in acidic environment during oral administration, to sustain the release, drug leakage during storage and low loading capacity. A modified solvent diffusion method in aqueous system was applied to prepare nanostructured lipid nanoparticles. Hydrophilic polymers such as chitosan and sodium alginate were used as coating materials. Glycerol mono oleate and oleic acid were used as solid and liquid lipid, respectively. Poloxamer is used as stabilizers. The central composite rotatable design consisting of three-factored factorial design with three levels was used in this study. The physiochemical characterization included evaluation of surface morphology, particle size and surface charge of the drug in the delivery system. The in vitro drug release, entrapment and drug loading efficiency and as well as the storage stability were evaluated. The results showed that the optimal formulation was composed of drug/lipid ratio of 1:3, organic/aqueous phase ratio of 1:10 and concentration of surfactant of 1 % w/v. Ifosfamide nanostructured lipid carrier under the optimized conditions gave rise to the entrapment efficiency of 77 %, drug loading of 6.14 %, mean diameter of 223 nm and zeta potential value of −25 mV. Transmission electron microscopy analysis showed spherical particles. The in vitro experiment proved that ifosfamide from the delivery system released gradually over the period of 72 h. Sodium alginate cross-linked chitosan nanostructured lipid carrier demonstrated enhanced stability of ifosfamide, high entrapment efficiency and sustained release.

Preparation and Characterization of Rizatriptan Benzoate Loaded Solid Lipid Nanoparticles for Brain Targeting

Solid lipid nanoparticles are at the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery. Due to their unique size dependent properties, lipid nanoparticles offer possibility to develop new therapeutics. The ability to incorporate drugs into nanocarriers offers a new prototype in drug delivery that could use for targeting of drugs to brain. The intra nasal formulation of rizatriptan benzoate would offer a practical non-invasive and an alternative route of administration for rapid drug delivery to brain and to treat migraine. Solid lipid nanoparticle containing poloxamer with mucoadhesive property increases the contact time at nasal mucosa, hence improved absorption of drug. Rizatriptan loaded solid lipid nanoparticles were prepared by modified solvent diffusion method and characterized for shape, surface morphology, particle size, FTIR, DSC, X-ray diffraction studies, drug entrapment, total drug content and in vitro drug release studies. These lipid nanoparticles were spherical in shape with smooth surface and possess particles of size range from 145 to 298nm. The maximum in vitro drug release was found to be 91% in 8hr, drug content was between 35-45% and maximum entrapment efficiency was 80%. In vivo studies were carried out on wistar rats and the estimation of rizatriptan benzoate was performed in cerebrospinal fluid and in blood and was conceived by HPLC method. Optimized formulation of solid lipid nano particles was given intranasally and compared with I.V and oral rote with equivalent dose. The optimized nasal SLN showed values of Cmax 473.56 ng/ml, Tmax 1hr, AUC 3706.95ng/ml and T1/2 was 5.7hr, that are more superior than marketed oral formulation and drug solutions given by iv route. Rizatriptan benzoate formulated as solid lipid nanoparticles for nasal administration could have potential to avoid first-pass effect than oral route, thus improve bioavailability of drug and as a safe and sustained release nasal delivery system to control migraine.

Surface Molecular Composition and Electrical Property of Cationic Solid Lipid Nanoparticles with Assembled Lipid Layer Mediated by Noncovalent Interactions

Understanding of charged groups on nanostructured lipid particles is an important issue in nanomedicine development. This study presents the relation between noncovalent interactions and the composition of ionogenic groups in the assembled lipid layer of cationic solid lipid nanoparticles (CSLNs). Innovated CSLNs containing cacao butter, cholesterol, stearylamine, and esterquat 1 (EQ 1) were fabricated by modified solvent diffusion method. The results revealed that the average diameter of CSLNs decreased when the weight percentage of cholesterol and EQ 1 increased. X-ray photoelectron spectroscopy and Fourier-transform infrared spectroscopy evidenced strong interactions between cholesterol and EQ 1. These noncovalent interactions exhibited hydrophobic and cation–aromatic characteristics and mediated the distribution of lipids in the external layer of CSLNs. In addition, an increase in the weight percentage of cholesterol and EQ 1 enhanced the zeta potential, electrophoretic mobility, and fixed charge density on CSLNs. The noncovalent interactions in the assembled lipid layer affect the chemical composition on the lipid surface and yield intriguing electrokinetic behavior of CSLNs.

Preparation of Magnetic Microspheres Based on Poly(<I>ε</I>-Caprolactone)-Poly(Ethylene Glycol)Poly(<I>ε</I>-Caprolactone) Copolymers by Modified Solvent Diffusion Method

Magnetic microspheres have promising application in biomedical field. In this paper, biodegradable poly(epsilon-caprolactone)-poly(ethylene glycol)-poly(epsilon-caprolactone) (PCEC) triblock copolymers were synthesized by ring-opening polymerization method. Through adjusting the epsilon-CL/PEG weight ratio in feed, PCEC copolymers with different block ratio were obtained. A novel modified solvent diffusion method was described to prepare magnetic PCEC composite microspheres containing magnetite nanoparticles. The particle size of microsphere decreased with increase in the PEG/PCL block ratio. The obtained microspheres could response to external magnetic field. This study described a novel method to prepare magnetic microspheres. The obtained magnetic polymeric microspheres might have potential application in drug delivery system or disease diagnosis field.

Preparation, characterization and taste-masking properties of microspheres containing azithromycin

Abstract Objectives The aim of this study was to prepare a microsphere formulation in order to mask the bitter taste of azithromycin. Methods Microspheres of azithromycin with ethyl cellulose were prepared by the modified solvent diffusion method. The microspheres were mixed with other excipients to form orally dry suspensions and the sensory test for taste masking was evaluated. Key findings Results demonstrated that the suspension could significantly mask the bitter taste of azithromycin and the relative bioavailability of suspensions to reference preparations was 102.7%. Conclusions The results indicate that the microsphere formulation can be a promising drug carrier for masking the bitter taste of azithromycin.

Preparation, characterization and taste-masking properties of microspheres containing azithromycin

The aim of this study was to prepare a microsphere formulation in order to mask the bitter taste of azithromycin. Microspheres of azithromycin with ethyl cellulose were prepared by the modified solvent diffusion method. The microspheres were mixed with other excipients to form orally dry suspensions and the sensory test for taste masking was evaluated. Results demonstrated that the suspension could significantly mask the bitter taste of azithromycin and the relative bioavailability of suspensions to reference preparations was 102.7%. The results indicate that the microsphere formulation can be a promising drug carrier for masking the bitter taste of azithromycin.

Drug/Dye‐Loaded, Multifunctional Iron Oxide Nanoparticles for Combined Targeted Cancer Therapy and Dual Optical/Magnetic Resonance Imaging

A biocompatible, multimodal, and theranostic functional iron oxide nanoparticle is synthesized using a novel water-based method and exerts excellent properties for targeted cancer therapy, and optical and magnetic resonance imaging. For the first time, a facile, modified solvent diffusion method is used for the co-encapsulation of both an anticancer drug and near-infrared dyes. The resulting folate-derivatized theranostics nanoparticles could allow for targeted optical/magnetic resonance imaging and targeted killing of folate-expressing cancer cells.