Spanlastics: a novel elastic drug delivery system with potential applications via multifarious routes of administration.

Drug delivery systems (DDS) based on nanocarriers are designed to transport therapeutic agents to specific areas of the body where they are required to exhibit pharmacodynamic effect. These agents rely on an appropriate carrier to protect them from rapid degradation or clearance and enhance their concentration in target tissues. Spanlastics, an elastic, deformable surfactant-based nanovesicles have the potential to be used as a drug delivery vehicle for wide array of drug molecules.

Levofloxacin loaded clove oil nanoscale emulgel promotes wound healing in Pseudomonas aeruginosa biofilm infected burn wound in mice.

Owing to their tolerance to antibiotics, bacterial biofilms continue to pose a threat to mankind and are leading cause for non-healing of burn wounds. Within the biofilm matrix, antibiotics become functionally inactive due to restricted penetration and enzymatic degradation leading to rise of antimicrobial resistance. The objective of present investigation was to develop and characterize levofloxacin (LFX) loaded clove oil nanoscale emulgel (LFX-NE gel) and evaluate its in vivo therapeutic efficacy in Pseudomonas aeruginosa biofilm infected burn wound in mice.

Engineered Site-specific Vesicular Systems for Colonic Delivery: Trends and Implications.

Steering drug-loaded, site-specific, coated lipid vesicles to the target receptor sites have the potential of plummeting adverse effects and improving the pharmacological response in diverse pathologies of the large bowel, especially the colon. Colonic delivery via oral route has its own challenges, often governed by several glitches such as drug degradation or absorption in the upper GIT, instability of proteins/peptides due to high molecular weight, and peptidase activity in the stomach. Consequently, colon-specific coated liposomal systems (CSLS) offer a potential alternate for not only site-specificity, but protection from proteolytic activity, and prolonged residence time for greater systemic bioavailability.

In Situ Forming Depot as Sustained-Release Drug Delivery Systems.

In situ forming systems can serve as promising alternative to existing long acting injectables like disperse systems and microspheres, owing to their biocompatibility, stability, ease of administration and scale up. Microspheres based on long-acting parenteral systems pose challenges in scaling up and process changes with the drug and polymer selected. In situ gelling systems are having low viscosity which is very conducive during various manufacturing unit operations and passing the formulation through hypodermic needle with lower applied pressure.

A New Therapeutic Approach for Brain Delivery of Epigallocatechin Gallate: Development and Characterization Studies.

Background: Blood-brain permeability is the primary concern when dealing with the biodistribution of drugs to the brain in neurological diseases.

Objective: The purpose of the study is to develop the nanoformulation of Epigallocatechin gallate (EGCG) in order to improve its bioavailability and penetration into the brain.

Methods: EGCG loaded Solid Lipid Nanoparticles (SLNs) have been developed using microemulsification method and pharmacological assessments were performed.

Enhancement of In Vivo Efficacy and Oral Bioavailability of Aripiprazole with Solid Lipid Nanoparticles.

Aripiprazole (ARP), a second-generation or atypical antipsychotic, is poorly soluble and undergoes extensive hepatic metabolism and P-glycoprotein efflux which lead to reduced in vivo efficacy and increased dose-related side effects. To enhance in vivo efficacy and oral bioavailability of aripiprazole, aripiprazole-loaded solid lipid nanoparticles (SLNs) were developed using tristearin as solid lipid. Tween 80 and sodium taurocholate were used as surfactants to prepare SLNs using microemulsification method.

Liquid Nanosize Emulsion-Filled Enteric-Coated Capsules for Colon Delivery of Immunosuppressant Peptide.

Present study aims at solubilizing slightly water-soluble peptide into a nanosize emulsion which is filled into a hard gelatin capsule in the form of preconcentrate. Further, liquid-filled capsule was dip-coated with ethyl cellulose and Eudragit S100 for colon targeting. An in vitro release profile was studied for selected formulations, i.

Effect of mesenchymal stem cells and galantamine nanoparticles in rat model of Alzheimer's disease.

Aim: The present study investigated the efficacy of bone marrow-derived mesenchymal stem cells (BM-MSCs) in combination with galantamine hydrobromide-loaded solid lipid nanoparticles (GH-SLNs) in intracerebroventricular (ICV)-isoproterenol-induced rat model of Alzheimer's disease.

Materials & Methods: BM-MSCs were harvested by dissecting femur and tibia of 8-10-week-old Wistar rats. 1 × 10(6) cells were administered intravenously once in ICV-isoproterenol-induced rats followed by GH-SLNs (5 mg/kg) for 3 weeks.

Evaluation of Ocular Irritation and Bioavailability of Voriconazole Loaded Microemulsion.

Background: Voriconazole (VCZ), a second-generation antifungal with excellent attributes like, broad-spectrum activity, targeted delivery, and tolerability. VCZ loaded microemulsion could be an effective strategy for efficient ocular delivery of the drug.

Objective: To perform corneal irritation studies and in vivo delivery of VCZ microemulsion to establish its potential as an efficient ocular delivery system.

Solid lipid nanoparticle: an efficient carrier for improved ocular permeation of voriconazole.

This research focuses on the fabrication and evaluation of solid lipid nanoparticles (SLNs) for improved ocular delivery of voriconazole (VCZ). Compritol and palmitic acid were selected as lipid carriers based on drug solubility and partitioning behavior. Poloxamer and soya lecithin were the choice for surfactant, while sodium taurocholate was used as a co-surfactant.

Emerging Potential of Nanosuspension-Enabled Drug Delivery: An Overview.

Poor aqueous solubility is one of the key concerns of the majority of new drug molecules. One of the important problems associated with such drugs is that they often lead to low bioavailability. Researchers have used various techniques, but little success has been achieved due to poor stability and industrial viability, including technique cost.

Design, Development and Characterization of Topical Microemulsions of 5-Fluorouracil for the Treatment of Non Melanoma Skin Cancer and its Precursor Lesions.

Treatment of non melanoma skin cancer and its precancerous skin lesions is associated with severe topical and systemic toxicity. So, it has become necessary to develop an efficient novel delivery system with less side effects and better patient compliance. Topical w/o microemulsion of 5-FU were prepared using sorbitan monooleate (Span 80), sorbitan trioleate (Span 85), polysorbate 80 (Tween 80), isopropyl alcohol (IPA) with different oils such as oleic acid, triacetin and isopropyl myristate (IPM).

Pioglitazone hydrochloride: chemopreventive potential and development of site-specific drug delivery systems.

The aim of this study was to investigate the potential of pioglitazone hydrochloride as a promising anticancer agent and then to design and evaluate the colon-targeted delivery system. The role of pioglitazone hydrochloride as a promising anticancer agent was evaluated by in vitro cell line studies and in vivo 1,2-dimethylhydrazine-induced colon carcinogenesis in rats. In order to deliver the drug at site of action, i.

Emergence of nanomedicine as cancer targeted magic bullets: recent development and need to address the toxicity apprehension.

Multi drug resistance and non specific targeting is a major problem with conventional therapy. To overcome this problem, nanoparticles (NPs) have emerged as an important tool to deliver conventional drugs, recombinant proteins, vaccines and more recently, nucleotides. NPs modify the drug release pattern, absorption, distribution, metabolism, excretion (ADME) and therapeutic response.

Utility of an oxidation reaction for the spectrophotometric determination of acarbose in controlled release tablets at various simulated gastrointestinal media.

A sensitive kinetic method for spectrophotometric determination of acarbose is developed and validated for the determination of the drug in bulk and pharmaceutical formulations. The drug was estimated in simulated gastrointestinal media i.e.

Newer insights into the drug delivery approaches of α-glucosidase inhibitors.

Introduction: α-Glucosidase inhibitors (AGIs) are an important category of oral antidiabetic agents being extensively exploited for the effective management of type 2 diabetes and associated disorders. These drugs significantly reduce the postprandial rise in glycemic and plasma insulin levels both in nondiabetics and in type 2 diabetic patients. Currently only three drugs belonging to this category, viz, acarbose, miglitol and voglibose are in the market.

A novel synergistic galactomannan-based unit dosage form for sustained release of acarbose.

In the current study, the potential of a novel combination of a galactomannan with acarbose (100 mg) was evaluated for attaining a desired hypoglycaemic effect over a prolonged period of time. Three major antidiabetic galactomannans viz., fenugreek gum, Boswellia gum, and locust bean gum were selected in order to achieve a synergistic effect in the treatment along with retardation in drug release.

Tailoring of drug delivery of 5-fluorouracil to the colon via a mixed film coated unit system.

The study was carried out to establish the effectiveness of a mixed film composed of ethylcellulose/Eudragit S100 for colonic delivery of 5-flourouracil (5-FU). Tablets cores containing 5-FU were prepared by direct compression method by coating at different levels (2-9%, m/m) with a non-aqueous solution containing ethylcellulose/Eudragit S100. Coated tablets were studied for the in vitro release of 5-FU and the samples were analyzed spectrophotometrically at 266 nm.

Nanoemulsions as self-emulsified drug delivery carriers for enhanced permeability of the poorly water-soluble selective β₁-adrenoreceptor blocker Talinolol.

Unlabelled: To enhance the bioavailability of the poorly water-soluble drug talinolol, a self-nanoemulsifying drug delivery system (SNEDDS) comprising 5% (w/v) Brij-721 ethanolic solution (Smix), triacetin, and water, in the ratio of 40:20:40 (% w/w) was developed by constructing pseudo-ternary phase diagrams and evaluated for droplet size, polydispersity index, and surface morphology of nanoemulsions. The effect of nanodrug carriers on drug release and permeability was assessed using stripped porcine jejunum and everted rat gut sac method and compared with hydroalcoholic drug solution, oily solution, and conventional emulsion and suspension. The SNEDDS showed a significant (P < 0.

Molecular simulation of hydroxypropyl-beta-cyclodextrin with hydrophobic selective Cox-II chemopreventive agent using host-guest phenomena.

The present investigation outlays the host-guest penetration of hydrophobic selective Cox-II chemopreventive agent, celecoxib (CXB), with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) using inclusion complexation phenomena. Phase solubility studies conducted at 37 degrees C and 25 degrees C revealed typical A(L)-type curve for the HP-beta-CD indicating the formation of soluble complexes. The inclusion complexes in the molar ratio of 1:1 and 2:1 (CXB-HP-beta-CD) were prepared by kneading technique.

In vivo bioavailability and therapeutic assessment of host-guest inclusion phenomena for the hydrophobic molecule etodolac: pharmacodynamic and pharmacokinetic evaluation.

The aim of present investigation was 1) to evaluate the in vivo bioavailability of an Etodolac (ETD)-Î-cyclodextrin (Î-CD) inclusion complex system prepared by kneading and spray drying techniques in rats, 2) to study the pharmacodynamic parameters in various animal models for analyzing the therapeutic response and, 3) to evaluate the pharmacokinetic profile of the drug administered. Inclusion complexation with Î-CD enhanced the solubility of the drug, improved bioavailability and reduced ulcerogenicity of ETD in rats. Pharmacodynamic studies were carried out in normal LACA mice and pharmacokinetic evaluation was done in male Wistar rats.

Development, characterization, and evaluation of ketorolac tromethamine-loaded biodegradable microspheres as a depot system for parenteral delivery.

Ketorolac tromethamine, a potent nonnarcotic analgesic agent and 800 times more potent than aspirin, is indicated for the short-term management of moderate to such severe painful states as post operative pain, acute musculoskeletal pain, and dental pain. It Given every 6 hr intramuscularly in patients for acute pain, to avoid frequent dosing and patient inconvenience Ketorolac from ethamine was found suitable for parenteral depot system by biodegradable microspheres for the present study. Ketorolac tromethamine-loaded microspheres were prepared by o/w emulsion solvent evaporation technique using different polymers viz.

Physicochemical characterization and in vitro dissolution behaviour of celecoxib-beta-cyclodextrin inclusion complexes.

In this study, attempts were made to investigate the effects of beta-cyclodextrin (beta-CD) on the aqueous solubility and dissolution rate of celecoxib. Inclusion complexes were prepared by the kneading method and characterized by SEM, NMR, IR, DSC, and X-ray powder diffraction. Dissolution rate of the complexes was significantly greater than that of the corresponding physical mixtures and pure drug, indicating that the formation of inclusion complex increased the solubility of the poorly soluble drug celecoxib.

Bioavailability of immediate- and extended-release formulations of glipizide in healthy male volunteers.

Background And Objective: An extended-release glipizide formulation using a hydrophilic matrix system containing hydrophilic polymers has been developed for use in diabetes mellitus. This study compared the pharmacokinetic parameters of immediate- and extended-release formulations of glipizide 5mg in healthy male volunteers.

Methods: In a single-dose, four-period, four-treatment, Latin-square crossover study, the bioavailability of immediate-release glipizide 5mg (Glynase) [GL], extended-release glipizide 5mg (Glynase) XL [GLXL], Glucotrol XL [GTXL], and the new formulation developed in our laboratory [GLPF]) was compared.

Formulation, characterization, and evaluation of ketorolac tromethamine-loaded biodegradable microspheres.

Ketorolac tromethamine has to be given every 6 hr intramuscularly in patients for acute pain, so to avoid frequent dosing and patient inconvenience we found it to be a suitable candidate for parenteral controlled delivery by biodegradable microspheres for the present study. Ketorolac tromethamine-loaded microspheres were prepared by o/w emulsion solvent evaporation technique using different polymers: polycaprolactone, poly lactic-co-glycolic acid (PLGA 65/35), and poly lactic-co-glycolic acid (PLGA 85/15). To tailor the release profile of drug for several days, blends of PLGA 65/35 and PLGA 85/15 were prepared with polycaprolactone (PCL) in different ratios.