Development and optimization of guaifenesin sustained release mini-tablets for adult and geriatric patients.

The main aim of this study was to formulate and optimize sustained release mini-tablets of guaifenesin. Guaifenesin granules were successfully prepared using different blend ratios of carnauba wax to drug by melt granulation method. The properties of granules were further modified by combining them with ethyl cellulose.

Development and characterization of bilayered tablets of diazepam for oral drug delivery: design, optimization and evaluation.

The oral bioavailability of drugs can be limited by their short residence time in the gastrointestinal tract. This study was performed to design bilayered floating tablets of diazepam comprising immediate-release and controlled-release layers. The tablets were prepared using sodium starch glycolate, polyvinyl pyrrolidone, hydroxypropyl methylcellulose and microcrystalline cellulose and evaluated for their characteristics.

Development and characterization of a novel mucoadhesive sol-gel suppository of sumatriptan: design, optimization, and evaluation for rectal drug delivery.

Sumatriptan (ST) is used for the treatment of migraine and cluster headaches. However, it exhibits low oral bioavailability (15%) due to the high first-pass metabolism. The aim of this work was to formulate an ST rectal hydrogel.

The Factors Determining the Skin Penetration and Cellular Uptake of Nanocarriers: New Hope for Clinical Development.

The skin provides a protective barrier against toxic environments and also offers a valuable route for topical drug delivery. The stratum corneum (SC) is the outermost layer of the skin and serves as the major barrier to chemical transfer through the skin. The human skin barrier is particularly difficult to overcome because of the complex composition and structure of the SC.

Preparation and optimization of fast disintegrating tablets of isosorbide dinitrate using lyophilization method for oral drug delivery.

Orally disintegrating tablets rapidly disintegrate in saliva and then swallowed without the need for water. The orally disintegrating tablets were prepared by freeze-drying of an aqueous dispersion of isosorbide dinitrate containing a matrix former (gelatin), a cryoprotectant (mannitol), a plasticizer (glycerin) and a dissolution enhancer (Tween/polyethylene glycol). Results demonstrated that the selected formulation, Ft, disintegrated within 1 min and showed faster dissolution rate compared with the commercial tablet.

Preparation and evaluation of thermosensitive and mucoadhesive hydrogels for intranasal delivery of phenobarbital sodium.

Recently, intranasal administration has been suggested as a potential direct route to transport pharmaceuticals into the brain through the olfactory and trigeminal nerves, bypassing the blood-brain barrier. The nasal hydrogels were prepared by a cold method using pluronic F-12 and chitosan. All the selected formulations were gelled at 30°C.

Expert Design and Optimization of Ethyl Cellulose-Poly (ε-caprolactone) Blend Microparticles For Gastro-Retentive Floating Delivery of Metformin Hydrochloride.

Background: Metformin Hydrochloride (MH) is an oral anti-hyperglycemic agent belonging to the biguanide class of drugs.

Objective: The present study involves the formulation and evaluation of gastro-retentive floating microparticles containing MH as a model drug for the prolongation of absorption time.

Methods: Three levels of a three-factor, Box-Behnken design were used to evaluate the critical formulation variables.

Development and characterization of sublingual films for enhanced bioavailability of selegiline hydrochloride.

Low oral bioavailability of selegiline hydrochloride (SH) is primarily due to extensive first-pass metabolism and hence the need for an alternative pathway of administration. Herein, we report the development of sublingual SH films. The films were formulated with varying polymer composition (F1-F6) and evaluated for physicochemical characteristics, drug release and permeation studies.

Expert design and optimization of a novel buccoadhesive blend film impregnated with metformin nanoparticles.

The purpose of this study was to design a metformin nanoparticles (NPs)-loaded buccoadhesive film for enhanced drug bioavailability. The NPs were prepared and incorporated into a hydroxypropyl methylcellulose-chitosan blend film. Three levels of a three-factor, Box-Behnken design were used to evaluate the critical formulation variables.

Preparation and characterization of cyclodextrin nanosponges for bortezomib delivery.

Background: Bortezomib (BTZ) as an anticancer drug has been used through the injection pathway.

Research Design And Methods: Two types of Cyclodextrin nanosponges (CDNSs) were synthesized and studied by DLS, TEM, FTIR, and DSC instruments for BTZ delivery. Both carriers were analyzed for loading efficiencies and release.

Desirability function approach for development of a thermosensitive and bioadhesive nanotransfersome-hydrogel hybrid system for enhanced skin bioavailability and antibacterial activity of cephalexin.

Cellulitis is a common bacterial infection of the skin and soft tissues immediately beneath the skin. Despite the successful use of antibiotics in the treatment of infectious diseases, bacterial infections continue to impose significant global health challenges because of the rapid emergence of antibiotic resistance. The aim of this work was to develop an hydrogel forming system containing highly permeable cephalexin-loaded nanotransfersomes (NTs), suitable for antibacterial drug delivery.

Preparation and characterization of a novel thermosensitive and bioadhesive cephalexin nanohydrogel: a promising platform for topical antibacterial delivery.

Objective: Impetigo is a common and highly contagious bacterial skin infection that mostly affects young children and infants. Herein, we report the development of a thermosensitive and bioadhesive hydrogel-forming system containing cephalexin-loaded nanoparticles (NPs) suitable for antibacterial drug delivery.

Methods: The nanohydrogel was formulated using drug-loaded NPs and characterized by its physicochemical characteristics.

PLA-PCL-PEG-PCL-PLA based micelles for improving the ocular permeability of dexamethasone: development, characterization, and evaluation.

The aim of the present research was to investigate the feasibility of developing polylactide-polycaprolactone-polyethylene glycol-polycaprolactone-polylactide (PLA-PCL-PEG-PCL-PLA) based micelles to improve ocular permeability of dexamethasone (DEX). PLA-PCL-PEG-PCL-PLA copolymers were synthesized by a ringopening polymerization method. DEX was loaded into the developed copolymers.

Formulation and Evaluation of Eudragit RL-100 Nanoparticles Loaded In-Situ Forming Gel for Intranasal Delivery of Rivastigmine.

Rivastigmine hydrogen tartrate (RHT) is commonly used for the treatment of mild to moderate Alzheimer's disease (AD). The aim of this work was to formulate in-situ pluronic F-127 (PF-127) hydrogels containing Eudragit RL-100 (EU-RL) nanoparticles (NPs) in order to improve the therapeutic efficacy of RHT through the nasal route. The NPs were prepared using different polymer to drug ratios and evaluated for their physicochemical characteristics, cellular uptake and in vitro cytotoxicity against lung adenocarcinoma cells (A459).

Expert design and desirability function approach for the development of diazepam thermally sensitive rectal gel.

The aim of the present work was to develop an thermosensitive rectal gel for diazepam by using Expert-design for improving three factors and a three-level process was formed by using a cold method. Response surface design was utilized to investigate the effect of independent variables like sodium chloride (NaCl, X1), poloxamer 407 (F-127, X2) and diazepam (X3), on different dependent variables such as gelation temperature, mucoadhesive strength, drug content, along with permeation and stability. The obtained results revealed that the addition of diazepam enhanced the gelation temperature of hydrogel while it decreased the gel strength and mucoadhesive force.

A brief overview on nano-sized materials used in the topical treatment of skin and soft tissue bacterial infections.

: Skin and soft tissue infections are a significant clinical problem that can happen anywhere on the body. Bacteria are the most common cause of skin and soft tissue infections in humans. Despite the fact that there is a lot of antimicrobial agents and antibiotics for elucidating bacterial infections, the prevention and control of infectious diseases continue to be one of the greatest challenges for public health worldwide.

Freeze-thaw-induced cross-linked PVA/chitosan for oxytetracycline-loaded wound dressing: the experimental design and optimization.

Oxytetracycline is an antibiotic for the treatment of the infections caused by Gram-positive and Gram-negative microorganisms. Among novel formulations applied for damaged skin, hydrogels have shown to be superior as they can provide a moist environment for the wound. The purpose of this study was to prepare and evaluate the hydrogels of oxytetracycline consisted of polyvinyl alcohol (PVA) and chitosan polymers.

Evaluation of anti-inflammatory impact of dexamethasone-loaded PCL-PEG-PCL micelles on endotoxin-induced uveitis in rabbits.

The aim of this study was to investigate the capability of polycaprolactone-polyethylene glycol-polycaprolactone (PCL-PEG-PCL) micelles in improving the anti-inflammatory effects of dexamethasone (DEX). A film hydration method was used for the preparation of the DEX-loaded PCL-PEG-PCL micelles. In vitro cytotoxicity of the micelles obtained was investigated on L929 cells.

Cyclodextrin-based nanosponges as promising carriers for active agents.

Introduction: In recent years, new drug delivery systems have attempted to overcome the undesirable pharmacokinetic problems of various drugs. Among them, cyclodextrin nanosponges (CDNSs) attract great attention from researchers for solving major bioavailability problems such as inadequate solubility, poor dissolution rate, and the limited stability of some agents, as well as increasing their effectiveness and decreasing unwanted side effects. This novel system can also be prepared as different dosage forms.

Box-Behnken experimental design for preparation and optimization of the intranasal gels of selegiline hydrochloride.

Selegiline hydrochloride (SL) is chosen as an adjunct for the control of clinical signs of Parkinsonian patients. The aim of the present work is to develop and optimize thermosensitive gels using Pluronic (F-127) for enhancing transport of SL into the brain through the nasal route. SL gels were prepared using a cold method and the Box-Behnken experimental design methodology.

Preparation and evaluation of PCL-PEG-PCL micelles as potential nanocarriers for ocular delivery of dexamethasone.

Objectives: Micelles have been studied as nanoparticulate drug delivery systems for improving the topical ocular delivery of hydrophobic drugs. The objective of this study was to develop and characterize dexamethasone-loaded polycaprolactone-polyethylene glycol-polycaprolactone (PCL-PEG-PCL) micelles to improve patient compliance and enhance the ocular bioavailability of poorly water-soluble drugs.

Materials And Methods: The PCL-PEG-PCL copolymers were synthesized via the ring opening polymerization of ε-caprolactone in the presence of PEG.

Novel Pentablock Copolymers as Thermosensitive Self-Assembling Micelles for Ocular Drug Delivery.

Many studies have focused on how drugs are formulated in the sol state at room temperature leading to the formation of in situ gel at eye temperature to provide a controlled drug release. Stimuli-responsive block copolymer hydrogels possess several advantages including uncomplicated drug formulation and ease of application, no organic solvent, protective environment for drugs, site-specificity, prolonged and localized drug delivery, lower systemic toxicity, and capability to deliver both hydrophobic and hydrophilic drugs. Self-assembling block copolymers (such as diblock, triblock, and pentablock copolymers) with large solubility variation between hydrophilic and hydrophobic segments are capable of making temperature-dependent micellar assembles, and with further increase in the temperature, of jellifying due to micellar aggregation.

Fabrication and Evaluation of Ketotifen Fumarate-loaded PLGA Nanoparticles as a Sustained Delivery System.

Ketotifen fumarate is a non-bronchodilator anti-asthmatic drug which inhibits the effects of certain endogenous substances known to be inflammatory mediators, and thereby exerts antiallergic activity. The present study describes the formulation of a sustained release nanoparticle (NP) drug delivery system containing ketoftifen, using poly (D,L lactide-co-glycolide) acid (PLGA). Biodegradable NPs were prepared using 50 : 50 PLGA by a water in-oil-in-water (w/o/w) double emulsion-solvent evaporation procedure and characterized for drug content, DSC (differential scanning calorimetry, XRD (X-ray diffractionl), FTIR (Fourier transform spectroscopy), particle size , surface morphology using scanning electron microscopy, and drug release rate.

Development of a nanoprecipitation method for the entrapment of a very water soluble drug into Eudragit RL nanoparticles.

Rivastigmine hydrogen tartrate (RHT), one of the potential cholinesterase inhibitors, has received great attention as a new drug candidate for the treatment of Alzheimer's disease. However, the bioavailability of RHT from the conventional pharmaceutical forms is low because of the presence of the blood brain barrier. The main aim of the present study was to prepare positively charged Eudragit RL 100 nanoparticles as a model scaffold for providing a sustained release profile for RHT.