Formulation and evaluation studies of BSA loaded chitosan nanoparticles by polymerization technique.

Aim: To prepare BSA loaded chitosan nanoparticles by polymerization technique and to study the effect of initiator concentration upon particle size, product yield, entrapment efficiency, loading capacity and drug release from the formulation. Methodology: In the present study BSA loaded chitosan nanoparticles were prepared by polymerization technique. Three formulations were prepared by varying the concentration of Initiator. The concentration of Initiator (Ammonium per sulphate) was maintained 1%, 2% 3% in formulation 1, Formulation 2 and Formulation 3 respectively. The effect of initiator concentration on Mean particle diameter, Drug content, entrapment efficiency, loading capacity, electrophoretic mobility and zeta potential was studied. Results and discussion: Best nanoformulations were obtained with Ammonium per sulphate 2 % concentration with Mean particle diameter of 441.7 nm. Electrophoretic mobility and Zeta potential value (-3.304 and -42.1) was also more among all chitosan formulations indicating greater stability. Conclusion: Hence Formulation 2 was considered to be the best Formulation for the preparation of BSA loaded Chitosan nanoparticles

Review on microspheres as a drug delivery carrier

A well designed controlled drug delivery system can overcome some of the problems of conventional therapy and enhance the therapeutic efficacy of a given drug .To obtain maximum therapeutic efficacy, it becomes necessary to deliver the agent to the target tissue in the optimal amount in the right period of time there by causing little toxicity and minimal side effects. There are various approaches in delivering a therapeutic substance to the target site in a sustained controlled release fashion. One such approach is using microspheres as carriers for drugs. In this article importance of microsphere as a novel drug delivery carrier to attain site specific drug delivery was discussed

Preparation of sodium alginate nanoparticles by desolvation technique using iso propyl alcohol as desolvating agent

Objective : The present study was undertaken to prepare and characterize drug loaded Sodium Alginate nanoparticles using Desolvation technique. The model drug chosen was Ibuprofen. Method : These nanoparticles were prepared by two methods i.e; Continuous addition method and intermittent addition methods in which the addition of desolvating agent was done at the rate of 1ml per minute and 1 ml per 5 minutes respectively. The optimized formulation developed using these two methods were characterized for particle size and stability. Results : The best method among two was determined by comparing the particle size and stability of the formulation using Particle Size analyzer and Zeta Sizer. Mean particle diameter and Zeta Potential was found to be 289.8 nm, -44.5 mV and 289.2 nm, -49.9 mV for the particles prepared by Continuous addition method and Intermittent addition method respectively. Conclusion: Intermittent addition method was concluded as the best method for the preparation of Ibuprofen loaded sodium alginate nanoparticles because of their smaller particle size and greater stability

A Comparative Study of Aspirin Loaded Bovine Serum Albumin Nanoparticles Prepared by Desolvation Technique Using Various Desolvating Agents

Aspirin is mainly used in the treatment of rheumatoid arthtitis and ankylosing spondylitis (AS). The dose of aspirin required for the treatment is 3 g / day in divided doses. In order to avoid chances of missing the dose of drug, it is better to formulate sustained release dosage forms. In the present study, aspirin loaded bovine serum albumin (BSA) nanoparticles were prepared by desolvation technique using various desolvating agents such as acetone, ethanol and sodium sulphate. A comparative study was made among the three desolvating agents (acetone, ethanol and sodium sulphate) and two methods (continuous addition method and intermittent addition method) to decide the best desolvating agent and the better method for preparation of aspirin nanoparticles by desolvation method. Continuous and intermittent addition methods were followed for the addition of desolvating agent to the aqueous solution of bovine serum albumin. Bovine serum albumin nanoparticles prepared by intermittent addition of ethanol was showing better results with the mean particle diameter of 209 nm, entrapment efficiency of 50% and loading capacity of 23%. The drug release was slow, extending over a period of 24 h. The curve fitting data revealed that the release followed the first-order kinetics. Higuchis and Peppas plots stated that Fickian diffusion controlled the pattern in all formulations. From the results it can be concluded that the method of intermittent addition was the better method and ethanol was the best desolvating agent for the preparation of aspirin nanoparticles by desolvation technique

Formulation and Evaluation of Letrozole Nanoparticles by Salting Out Technique and Determination of Anti-cancer Activity by MTT Assay

ObjectiveLetrozole (LTZ) drug is an aromatase inhibitor used for the treatment of hormonally positive breast cancer in postmenopausal women. It has poor water solubility, rapid metabolism and a range of side effects. In this study, polymer-based nanoparticles (NPs) incorporating the drug have been formulated and evaluated, aimed to control the release, potentially maximize the therapeutic efficiency, and minimize the side effects of the drug.MethodologyThe drug is incorporated into the polymer (i.e., Eudragit S 100 and Ethyl cellulose) by employing the salting out technique. Total twelve formulations were prepared by varying drug-polymer concentrations and organic to aqueous phase ratios and evaluated for percentage yield, drug content and invitro drug release studies. Out of 12 formulations, the best formulations were selected based on drug content and invitro drug release studies and characterized for mean particle diameter and zeta potential.ResultsAmong all the twelve formulations F5EC, 1:2 was considered to be the best formulation with minimum particle size of 194.55 nm, zeta potential value of –18.6 mV, drug content of 90.28%, entrapment efficiency of 92.36%, and invitro drug release of 95% within 12 h. The drug release kinetic studies of the best formulations indicated that the release of drug followed zero order kinetics and showed non-fickian diffusion mechanism. Based on the evaluation and characterization of the formulations, the best formulation prepared by salting out technique (F5EC 1:2) was considered for the determination of anti-cancer activity invitro in MCF-7 breast cancer cell line by MTT assay. The results indicated that the prepared formulation exhibited anti-cancer activity with an IC50 value of 49.63 ng.ConclusionFinally, by comparing results, Ethyl cellulose (EC) was considered to be most suitable for the preparation of LTZ NPs by salting out technique. The Entrapment Efficiency of LTZ NPs was improved up to 92.36% by using salting out technique

PREPARATION AND CHARACTERISATION OF IBUPROFEN LOADED POLYMERIC NANOPARTICLES BY SOLVENT EVAPORATION TECHNIQUE

Objective: In the present study Ibuprofen loaded nanoparticles were prepared by solvent evaporation technique. Comparative study was done among the formulations to know the best stabilizer and the polymer for ibuprofen loaded nanoparticles. Methods: Four formulations F1, F2, F3 and F4 were prepared by solvent evaporation technique by changing the polymers and the stabilizers. The polymers used were Ethyl cellulose and Eudragit S-100 and the stabilizers were tween 80 and 0.4% PVA.The drug and the polymers was dissolved in solvent mixture of DCM and methanol in 1:1 ratio and added to the aqueous stabilizers. Comparative study was done to know the better formulation for EC with 0.4% PVA and tween 80, and also for Eudragit S-100 with Tween 80 and 0.4%PVA.Further Comparative study was performed between the best formulation of EC (F2) and Eudragit S-100 (F3).The effect of stabilizer and the polymer on nanoparticle size, stability, loading capacity, encapsulation efficiency and In vitro drug release was studied. Results: Ibuprofen nanoparticles.F1,F2,F3 and F4 were prepared by using EC with tween 80 and 0.4% PVA and Eudragit with the same stabilzers. The particle size and stability of the formulations was determined by Horiba SZ 100 series particle size analyzer. Encapsulation efficiency and loading capacity were determined by ELTEK NP 400 Ultracentrifuge. The drug content was found to be 87%,88.72%,81.05% and 80.6%,encapsulation efficiency was found to be 56.25%,88.36%,71.7% and 55.9 %,loading capacity was found to be 28.8%,39.2%,33% and 28.4% respectively for F1,F2,F3 and F4. The average particle size was found to be 320.9 nm for F2 and 694.8 nm for F3.The zeta potential was found to be optimum for both the formulations. Conclusions: On comparison F2 was considered to be the best formulation for the preparation of Ibuprofen loaded nanoparticles because of the smaller particle size and greater stability, greater loading capacity and encapsulation efficiency. The drug release was sustained till 8 hrs for nanoparticles in F2

Formulation and Evaluation of Etoricoxib Niosomes by Thin Film Hydration Technique and Ether Injection Method

The main objective of this study is to formulate etoricoxib niosomes as vesicular carriers for site specific drug delivery. Niosomes are novel vesicular carriers, in which the drug is incorporated in a vesicle. Niosomal vesicles are formed by hydrating mixture of cholesterol and nonionic surfactants. Niosomes can increase the permeability of the skin (stratum corneum and epidermis), by avoiding the first pass metabolism and also reduce the side effects. Etoricoxib is a potent new COX-2 inhibitor used in the treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute gout arthritis etc. Two formulations were prepared by thin film hydration technique using the drug, cholesterol and surfactants Tween 80 (F1) and Span 60 (F2). Another two formulations were prepared by ether injection method using cholesterol and surfactants Tween 80 (F3) and Span 60 (F4). Each formulation was evaluated for drug content, entrapment efficiency, mean vesicular diameter, zeta potential and In-vitro drug release studies. Among the four formulations, F2 formulation containing the drug and Span 60 showed maximal drug content of 95.57%, entrapment efficiency of 96.40%, mean vesicular diameter of 463.7 nm, zeta potential of –80.5 mV, in-vitro drug release of 95.14% in 12 h, and the drug release followed the first order with non-fickian diffusion mechanism by thin film hydration technique. Hence, the thin film hydration technique is an optimized technique for the preparation of etoricoxib niosomes

Formulation and Evaluation of Cox-2 Inhibitor (Etoricoxib) Loaded Ethyl Cellulose Nanoparticles for Topical Drug Delivery

The aim of this investigation was to formulate, characterize and evaluate etoricoxib (ET) loaded polymeric nanoparticles for topical delivery. For nanoprecipitation method, ethyl cellulose (EC) was used as polymers. All the formulations were prepared by varying the drug and polymer concentrations. The obtained nanoparticles were evaluated for yield, drug content, entrapment efficiency, loading capacity and in-vitro drug release. Comparative study was performed among the formulations of ethyl cellulose. For the formulation of the gel, carbopol 934 was used as a gelling base. By comparison, F3 formulation of ethyl cellulose was found to be the best with the highest entrapment efficiency of 79.1%, the smallest mean particle diameter (538 nm), a higher stability (–43.8 mV) and the ability to control the release for 12 h with 87.1% drug release. F3 formulation was incorporated into gel F3G. Based on the results, it could be concluded that F3G formulation of etoricoxib topical gel prepared with ethyl cellulose was found to be more efficient with the highest spreadability of 41.22 g.cm/sec and was able to sustain the drug release for about 12 h with a cumulative release of 79.1%

Preparation and Characterization of Naproxen Loaded Niosomes by Ether Injection Method

The objective of the present research was to prepare and characterize naproxen loaded niosomes by ether injection method. A total of sixteen formulations were prepared by ether injection method by varying the type and concentration of surfactant. All the formulations were evaluated for drug content, entrapment efficiency, loading capacity and drug release profiles. Based on evaluation parameters, formulation E14 prepared by ether injection method showed entrapment efficiency of 95.86%, drug content of 94.9%, zeta potential value of?31.9 mV, suggesting its higher stability and particle diameter of about 393.9 nm. In-vitro release studies also showed that of all the formulations, E14 released about 88.9% by the end of 12 hours, showing a sustained release pattern with high amount of drug release when compared to the other formulations. Drug release kinetic studies of optimized formulation (E14) followed zero order release with R2 value of 0.987 and showed super case 2 transport mechanism. Based on the results, tween 80 with 1:1 ratio of drug to surfactant was considered as the best formulation for the preparation of naproxen loaded niosomes by ether injection method

Formulation of Mefenamic Acid Loaded Ethosomal Gel by Hot and Cold Methods

The aim of the present study is the formulation of mefenamic acid ethosomal gel by hot and cold methods. To prepare the mefenamic acid transdermal gel, ethosomes was selected as colloidal carriers. Ethosomes were prepared by cold and hot methods. The obtained ethosomes were characterized with vesicular diameter, zeta potential, drug content, entrapment efficiency and in-vitro diffusion studies. The five formulations of ethosomes prepared by cold and hot methods were compared. Among the 10 formulations of ethosomes, E5 was considered as the best formulation because of its mean vesicular diameter of 854 nm, zeta potential of 20 mV, drug content of 96.3%, entrapment efficiency of 94.4%, sustained drug release for 12 hr, i.e. 94.4. Then the E5 formulations was incorporated into gel. A comparative study was made between the plain gel and the ethosomal gel. The Ethosomal gel was considered the best because of its highest drug content spreadability , pH (6.9) and the sustained drug release profile for 12 hr. By comparison, the cold method shows better results