FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF CIPROFLOXACIN BY SOLVENT EVAPORATION METHOD USING DIFFERENT POLYMERS

Objective: The main intention of this research was to formulate and evaluate floating microspheres of ciprofloxacin using different polymers to prolong gastric residence time. Methods: The microspheres were formulated by the solvent evaporation method using different ratios of polymers like carbopol 940, ethylcellulose, and Hydroxy Propyl Methyl Cellulose K4M. Further, the floating microspheres were evaluated for micromeritic properties like bulk density, tapped density, angle of repose, etc., percentage yield, particle size, entrapment efficiency, floating capacity, in vitro drug release study, release kinetics, drug content, swelling index, and Fourier Transform Infrared Spectroscopy (FTIR) (Compatibility studies). Results: The ciprofloxacin microspheres showed the good flowing property. The particle size ranged from 258.1±2.21 µm to 278±2.86 µm and entrapment efficiency ranged from 63.17±0.43% to 89.90±1.32%. The IR spectrum revealed that there was no interaction between the drug and polymer. F7 formulation was found to be the best formulation. Drug release was found to be 90.70±0.89% i.e. in a controlled manner at the end of 10 h. Conclusion: The floating microspheres were prepared successfully and the results clearly stated that prepared ciprofloxacin microspheres may be safe and effective controlled drug delivery over an extended period which can increase bioavailability, patient compliance, and decrease dosing frequency

FORMULATION OF SOLID DISPERSIONS FOR ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF SIMVASTATIN

Objective: The objective of the present work was to formulate the solid dispersions of simvastatin for enhancement of its aqueous solubility and dissolution rate. Methods: In the present study, solid dispersions of simvastatin were prepared by Kneading and Solvent evaporation methods. The polymeric carriers like Polyethylene glycol (PEG) 6000 and Polyvinyl Pyrrolidone (PVP) K30 were used in different ratios (ratio of drug: carrier was 1:1, 1:2) to formulate solid dispersions. The prepared solid dispersions were characterized by differential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FTIR), and evaluated for drug content, percentage yield, saturation solubility, in vitro dissolution studies. The best formula of the solid dispersion was selected according to the solubility and dissolution data. Results: The F7 formulation was found to be an optimized formulation containing PVP K30 in the ratio 1:1 prepared by solvent evaporation technique. The Drug content was found to be higher i.e. 94.89 in the F7 batch. The FT-IR spectra revealed that there was no interaction between drugs and carriers. DSC thermogram indicated entrapment of simvastatin in PVP K30 and the conversion of crystalline simvastatin into an amorphous form. The F7 formulation showed maximum drug release i.e. 98.60% in 60 min which is 2 times greater than pure drug making it an optimized formulation. Conclusion: The solubility of simvastatin was successfully enhanced through the solid dispersion technique. Solid dispersions prepared with solvent evaporation method were more soluble than solid dispersions prepared with kneading method with carrier PVP K30

Formulation and evaluation of thermoreversible mucoadhesive nasal gels of metoclopramide hydrochloride

The prolonged residence of drug formulation in the nasal cavity is of utmost importance for intranasal drug delivery. The objective of the present investigation was to develop a mucoadhesive in situ gel with reduced nasal mucocilliary clearance in order to improve the bioavailability of the antiemetic drug, metoclopramide hydrochloride. The in situ gelation upon contact with nasal mucosa was conferred via the use of the thermogelling Pluronic flake 127 (18%). Mucoadhesion was modulated via the use of hydroxy propyl methyl cellulose (HPMC), sodium carboxy methyl cellulose (Na CMC) and sodium alginate (Na-alginate) whereas drug release was modified by varying concentrations of polyethylene glycol 6000 (PEG 6000). The results revealed that the different mucoadhesives increased the gel viscosity but reduced its sol gel transition temperatures. The increase in viscosity was highest in formulations with Na-alginate and lowest in formulations with HPMC. PEG 6000 significantly decreased mucoadhesive strength of formula containing 0.3% HPMC (776.6 ± 19.55 to 713.6 ± 5.03), 0.2% Na CMC (656 ± 11.13 to 575 ± 9.07) and 0.2% Na-alginate (659 ± 11.13 to 618.3 ± 9.45) whereas the gelation temperature increased by 3 to 4 °C. 100% of drug diffusion was found at four hours for formulation F5, F9, and F12. Formulation F5 showed maximum permeability (0.00949 ± 0.00021 mg.cm/min) than other formulation containing PEG6000. This study concluded the potential use of mucoadhesive in situ nasal gel in terms of ease of administration, accuracy of dosing, prolonged nasal residence and improved nasal bioavailability.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation and evaluation of thermoreversible mucoadhesive nasal gels of metoclopramide hydrochloride

The prolonged residence of drug formulation in the nasal cavity is of utmost importance for intranasal drug delivery. The objective of the present investigation was to develop a mucoadhesive in situ gel with reduced nasal mucocilliary clearance in order to improve the bioavailability of the antiemetic drug, metoclopramide hydrochloride. The in situ gelation upon contact with nasal mucosa was conferred via the use of the thermogelling Pluronic flake 127 (18%). Mucoadhesion was modulated via the use of hydroxy propyl methyl cellulose (HPMC), sodium carboxy methyl cellulose (Na CMC) and sodium alginate (Na-alginate) whereas drug release was modified by varying concentrations of polyethylene glycol 6000 (PEG 6000). The results revealed that the different mucoadhesives increased the gel viscosity but reduced its sol gel transition temperatures. The increase in viscosity was highest in formulations with Na-alginate and lowest in formulations with HPMC. PEG 6000 significantly decreased mucoadhesive strength of formula containing 0.3% HPMC (776.6 ± 19.55 to 713.6 ± 5.03), 0.2% Na CMC (656 ± 11.13 to 575 ± 9.07) and 0.2% Na-alginate (659 ± 11.13 to 618.3 ± 9.45) whereas the gelation temperature increased by 3 to 4 °C. 100% of drug diffusion was found at four hours for formulation F5, F9, and F12. Formulation F5 showed maximum permeability (0.00949 ± 0.00021 mg.cm/min) than other formulation containing PEG6000. This study concluded the potential use of mucoadhesive in situ nasal gel in terms of ease of administration, accuracy of dosing, prolonged nasal residence and improved nasal bioavailability.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation and evaluation of thermoreversible mucoadhesive nasal gels of metoclopramide hydrochloride

The prolonged residence of drug formulation in the nasal cavity is of utmost importance for intranasal drug delivery. The objective of the present investigation was to develop a mucoadhesive in situ gel with reduced nasal mucocilliary clearance in order to improve the bioavailability of the antiemetic drug, metoclopramide hydrochloride. The in situ gelation upon contact with nasal mucosa was conferred via the use of the thermogelling Pluronic flake 127 (18%). Mucoadhesion was modulated via the use of hydroxy propyl methyl cellulose (HPMC), sodium carboxy methyl cellulose (Na CMC) and sodium alginate (Na-alginate) whereas drug release was modified by varying concentrations of polyethylene glycol 6000 (PEG 6000). The results revealed that the different mucoadhesives increased the gel viscosity but reduced its sol gel transition temperatures. The increase in viscosity was highest in formulations with Na-alginate and lowest in formulations with HPMC. PEG 6000 significantly decreased mucoadhesive strength of formula containing 0.3% HPMC (776.6 ± 19.55 to 713.6 ± 5.03), 0.2% Na CMC (656 ± 11.13 to 575 ± 9.07) and 0.2% Na-alginate (659 ± 11.13 to 618.3 ± 9.45) whereas the gelation temperature increased by 3 to 4 °C. 100% of drug diffusion was found at four hours for formulation F5, F9, and F12. Formulation F5 showed maximum permeability (0.00949 ± 0.00021 mg.cm/min) than other formulation containing PEG6000. This study concluded the potential use of mucoadhesive in situ nasal gel in terms of ease of administration, accuracy of dosing, prolonged nasal residence and improved nasal bioavailability.Colegio de Farmacéuticos de la Provincia de Buenos Aire

A Comprehensive Review on Floating Drug Delivery System (FDDS)

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and non-toxic for a prolonged period. Current pharmaceutical scenario focuses on the formulation of floating drug delivery system (FDDS). FDDS are low density systems that float over the gastric contents and remain buoyant in the stomach for a prolonged period of time without affecting the gastric emptying rate. The aim of writing this review is to compile the current literature with special focus on the principal mechanism of floatation to attain gastric retention. Effervescent FDDS release CO2 gas, thus reduce the density of the system and remain buoyant in the stomach for a prolonged period of time and released the drug slowly at a desired rate so it can be used to prolong the gastric residence time in order to improve the bioavailability of drug. The review briefly describes the mechanism, types of floating system, advantages, limitation, factors affecting floating system, drug candidates suitable for floating, evaluation parameters and application of the system. These systems are useful to several problems encountered during the development of a pharmaceutical dosage form and the future potential of FDDS. Keywords: Floating drug delivery system, Absorption Window, Effervescent system, floating lag time

As Review on Microsponge Gel as Topical Drug Delivery System

Microsponges are drug delivery systems composed of porous microspheres. They are little sponge – like spherical particles with an outside surface porous surface. Moreover, they will enhance stability, scale back aspect effect and modify drug unharness favourably. Microsponge technology has several favorable characteristics that make it a flexible drug delivery vehicle. Microsponge  system square measure supported microscopic, chemical compound based mostly microspheres that may suspend or entrap a good type of substances, and might may be incorporated into a developed product like a gel, cream, liquid, powder. The outer surface is often porous, permeating a sustained flow of drugs out of sphere. Microsponges square measure porous, compound microspheres that square measure used principally for typical use and have recently been used for oral administration. microsponge  square measure designed to deliver a pharmaceutical active ingredient with efficiency at the minimum dose and additionally to reinforce solubility, scale back aspect effects and modify drug unharness. Kyewords: Controlled release, drug delivery, care systems, microponges

Niosomes: A Novel Carrier Drug Delivery System

Niosomes are a novel drug delivery system, in which the medication is encapsulated in a vesicle. The vesicle is composed of a bilayer of non-ionic surfactants. Niosomes are mostly preferred than liposomes because they are stable and cost effective. Niosomes potentiate the pharmacological action of the drug molecules by delaying the clearance of the drug from the circulation, protecting the drug from biological environment and restricting the effects only to the target cells. In novel drug delivery it has applications on treatment of cancer, used as a carrier in haemoglobin, delivery of the peptide drugs through oral route, in treatment of leishmaniasis, in ophthalmic delivery and as carrier in dermal drug delivery. This review article focuses on the composition, advantages, types of niosomes, methods of preparation, characterization and application of the vesicular system. Keywords: Niosomes, Composition, Types, Method of preparation, Factors affecting, Application

Microsponge as an Emerging Technique in Novel Drug Delivery System

Numbers of developments are implemented in drug delivery system to achieve the goals of optimized efficacy, cost effectiveness of therapy. One of the latest, novel and highly evolving technologies is microsponge drug delivery system which gives controlled release and site specific delivery of active ingredients. They are highly cross linked, porous and polymeric microspheres with size range of 5-300µm. This system is emerging as valuable option for topical delivery of drugs due to characteristics like decreased side effects, improved stability, better formulation flexibility, superior product performance. It is having number of applications in oral, topical, ocular and biopharmaceuticals delivery. The current review describes microsponge technology and details of the formulation methods, evaluation, programmable release mechanisms and applications.   Keywords: Microsponges; Controlled release; Quasi emulsion solvent diffusion; Programmable drug release; Oral administration; Topical drug delivery