International Journal of Pharmaceutical Investigation

OBJECTIVE: The objective of the present work was to prepare and evaluate a novel oral formulation for systemic delivery of low molecular weight heparin (LMWH). The formulation consisted of Eudragit S 100-coated positively charged liposomes encapsulating LMWH and a penetration enhancer. MATERIALS AND METHODS: Positively charged liposomes were first prepared by the thin film hydration method using lipid (soy phosphotidylcholine and cholesterol) and stearyl amine (SA) in the optimum ratio of 16:1, along with cetylpyridinium chloride (CPC) as a penetration enhancer...

BACKGROUND: The purpose of this study was to develop ibuprofen (IB)-polyethylene glycol (PEG) 8000 solid dispersions (SDs) and investigate them for in vitro dissolution and in vivo anti-inflammatory activity. MATERIALS AND METHODS: IB-PEG 8000 SDs were prepared by fusion method using varying combination ratios of IB and PEG 8000. Characterization based on surface morphology, particle size, absolute drug content, and Fourier transform infrared (FT-IR) spectroscopy was carried out on the SDs...

The application of quality by design (QbD) in pharmaceutical product development is now a thrust area for the regulatory authorities and the pharmaceutical industry. International Conference on Harmonization and United States Food and Drug Administration (USFDA) emphasized the principles and applications of QbD in pharmaceutical development in their guidance for the industry. QbD attributes are addressed in question-based review, developed by USFDA for chemistry, manufacturing, and controls section of abbreviated new drug applications...

INTRODUCTION: The potent antifungal agent amphotericin B (AmB) is not freely soluble in water. The clinical use of AmB is limited by nephrotoxicity and poor water solubility. Polyamidoamine (PAMAM) dendrimer offers an identical carrier for drug binding that has the capacity to attach and discharge drugs in numerous ways. MATERIALS AND METHODS: In this research work, we explored the potential of PAMAM dendrimers to improve the solubility of AmB. RESULTS AND DISCUSSION: The experimental results indicated that the solubility of AmB was greatly enhanced in the presence of PAMAM dendrimer solutions...

INTRODUCTION: Oral sustained release gastro retentive dosage forms offer several advantages for drugs having absorption from the upper gastrointestinal tract to improve the bioavailability of medications which have narrow absorption window. The aim of the study was to develop a floating bioadhesive drug delivery system exhibiting a unique combination of floatation and bioadhesion to prolong the residence in the stomach using atenolol as a model drug. METHODS: Prior to compression, polymeric blend(s) were evaluated for flow properties...

BACKGROUND: The present research work was aimed at localization of fluconazole in the oral cavity by preferential coating of buccoadhesive tablet for the treatment of oral thrush. MATERIALS AND METHODS: In order to achieve the aim, buccoadhesive tablets were optimized using 3(2) full factorial design to study the influence of varying content of chitosan and carbopol 934P (input variables) on the responses. RESULTS: Perturbation plots revealed high sensitivity of the input variables to ex vivo mucoadhesion force and percent cumulative drug release (CDR) whereas the ex vivo mucoadhesion time was less sensitive to the input variables...

INTRODUCTION: Superiority of topical instillation of drug into the cul-de-sac for the treatment of various ophthalmic complications can be validated with commercial availability of a large number of conventional formulations even though this mode of instillation still elicits limitations owing to poor ocular bioavailability. To overcome the drawbacks of conventional formulations, a large number of novel carriers have been investigated. In this perspective, a new novel nanocarrier, chondroitin sulfate (ChS)-chitosan (CS)-nanoparticles (NPs) are being evaluated for improved delivery of bromfenac sodium...

INTRODUCTION: The aim of this study is to evaluate gatifloxacin-loaded sodium alginate hydrogel membranes, supplemented with glycerol (a plasticizer), glutaraldehyde (a cross-linking agent), and hydroxypropyl methylcellulose (HPMC) or hydroxypropyl cellulose (HPC) polymers, as potential wound dressing materials based on their physicochemical properties and the sustain-release phenomenon. MATERIALS AND METHODS: The physicochemical properties of the prepared hydrogel membranes were evaluated by several methods including Fourier transform infrared and differential scanning calorimetry...

In this study, thermosensitive, water-soluble, and biodegradable triblock copolymer PCL600-PEG6000-PCL600 was used to form supramolecular hydrogel (SMGel) by inclusion complexation with γ-cyclodextrin (γ-CD). The prepared SMGel was investigated as a carrier for sustained release of dexamethasone. The triblock copolymer PCL-PEG-PCL [where PCL = polycaprolactone, PEG = poly(ethylene glycol)] was synthesized by the ring-opening polymerization method using microwave irradiation. The polymerization reaction and the copolymer structures were evaluated by nuclear magnetic resonance (NMR) and gel permeation chromatography (GPC)...

INTRODUCTION: The aim of this study was to use Eudragit(®) RL 100 (pH-independent polymer) and magnesium stearate (a hydrophobic droplet stabilizer) in combination to improve the controlled release effect of insulin-loaded Eudragit(®) entrapped microspheres prepared by the emulsification-coacervation technique. MATERIALS AND METHODS: Mucoadhesive insulin-loaded microspheres containing magnesium stearate and varying proportions of Eudragit(®) RL 100 were prepared by the emulsification-coacervation technique and evaluated for thermal properties, physicochemical performance, and in vitro dissolution in acidic and subsequently basic media...

INTRODUCTION: Solubility and dissolution of a poor water-soluble drug are the two major barriers for formulation scientists in development of drug delivery. Many of the potent drugs do not show the therapeutic effects due to solubility issues but may show toxicity issues when used in high doses. Solid dispersion (SD) technology is an excellent tool for enhancing the solubility and dissolution and hence related bioavailability. MATERIALS AND METHODS: SD of spironolactone (SPL) was developed using an inert carrier polyethylene glycol 4000 (PEG 4000) by the conventional fusion method and characterized for various characterization parameters...

In the present investigation, solid lipid nanoparticles (SLNs)-loaded in situ gel with voriconazole drug was formulated. Further, the formulation was characterized for pH, gelling capacity, entrapment efficiency, in vitro drug release, drug content, and viscosity. Voriconazole is an antifungal drug used to treat various infections caused by yeast or other types of fungi. Film hydration technique was used to prepared SLNs from lecithin and cholesterol. Based on the entrapment efficiency 67.2-97.3% and drug release, the optimized formulation NF1 of SLNs was incorporated into in situ gels...

OBJECTIVE: The objective of the present investigation was formulation, optimization and characterization of mucoadhesive film of clotrimazole (CT) which is patient-convenient and provides an effective alternative for the treatment of vaginal candidiasis. CT is an antimycotic drug applied locally for the treatment of vaginal candidiasis. MATERIALS AND METHODS: Mucoadhesive vaginal films were prepared by solvent casting technique using hydroxyl propylcellulose and sodium alginate as polymers...

INTRODUCTION: This study focused on the potential effects of compression forces experienced during lactose (InhaLac 70, 120, and 230) storage and transport on the flowability and aerosol performance in dry powder inhaler formulation. MATERIALS AND METHODS: Lactose was subjected to typical compression forces 4, 10, and 20 N/cm(2). Powder flowability and particle size distribution analysis of un-compressed and compressed lactose was evaluated by Carr's index, Hausner's ratio, the angle of repose and by laser diffraction method...

BACKGROUND: The aim of this study was to formulate solidified reverse micellar solution (SRMS)-based solid lipid microparticles (SLMs) using homolipids from tallow fat (Bos indicus) and evaluate its potential for enhanced delivery of gentamicin. MATERIALS AND METHODS: SLMs were formulated by melt-emulsification using SRMS (15% w/w Phospholipon(®) 90G in 35% w/w Bos indicus), polyethylene glycol 4000 (PEG) and gentamicin (1.0, 2.0, 3.0% w/w), and characterized with respect to size, morphology, encapsulation efficiency % and pH-dependent stability...

Composite transdermal films of chitosan (CS)/montmorillonite K 10 (MMT) clay were prepared for the delivery of curcumin. CS/MMT films were evaluated for various physicochemical parameters. The films were characterized by Fourier transform infrared spectroscopy and X-ray diffraction analysis. Water uptake and swelling ratio of the films was found to decrease with increase in concentration of clay. Mechanical properties of the films were assessed in terms of tensile strength and extensibility using texture analyzer...

AIM: The aim was to develop a novel excipient from Pleurotus tuber-regium (PT)-cornstarch (CS) mixture and evaluate its multifunctional characteristics in tablet formulation. MATERIALS AND METHODS: Composites were generated from dephytochemicalized PT and CS combined at 1:1 to 4:1 ratios and pregelatinized in a hot water bath at 65°C ± 2°C for 5 min. The paste was dried, pulverized, and screened through 150-μm sieve. PT-CS physical mixtures were prepared and their characteristics/functionalities in tableting chloroquine were compared to those of composites and microcrystalline cellulose (Avicel(®))...

Many patients with advanced type 2 diabetes mellitus (T2DM) and all patients with T1DM require insulin to keep blood glucose levels in the target range. The most common route of insulin administration is subcutaneous insulin injections. There are many ways to deliver insulin subcutaneously such as vials and syringes, insulin pens, and insulin pumps. Though subcutaneous insulin delivery is the standard route of insulin administration, it is associated with injection pain, needle phobia, lipodystrophy, noncompliance and peripheral hyperinsulinemia...

INTRODUCTION: Choline bitartrate (CBT) is a vital nutrient for fetal brain development and memory function. It is hygroscopic in nature which is associated with stability related problem during storage such as development of fishy odor and discoloration. AIM: Microencapsulation method was adopted to resolve the stability problem and for this hydrogenated soya bean oil (HSO) was used as encapsulating agent. MATERIALS AND METHODS: Industrially feasible modified extrusion-spheronization technique was selected for microencapsulation...

INTRODUCTION: The objective of the present investigation was to develop a novel multifunctional directly compressible co-processed excipient consisting of dibasic calcium phosphate anhydrous, polyethylene glycol 4000 (PEG 4000) and crospovidone using Box-Behnken design. MATERIALS AND METHODS: The technique of melt granulation was adopted for the preparation of the co-processed excipient. The percentage of crospovidone (5-10% w/w), percentage of PEG 4000 (5-15% w/w) and the heating time (4-12 min) were selected as independent variables...