Drug-polymer Ratio Research Articles

Synthesis and Characterization of a Novel pH-Sensitive Aluminum Crosslinked Carboxymethyl Tragacanth Beads for Extended and Enteric Drug Delivery

Carboxymethyl tragacanth (CM-TG) with a DS of 1.2 was synthesized and characterized for drug delivery using diclofenac sodium as a model drug. The mixture of CM-TG and drug was ionically crosslinked using aluminum chloride to form drug-loaded beads. The concentrations of 10 and 20% w/w solution of CM-TG were found to produce beads with acceptable qualities. The beads exhibited pH-dependent swelling. The highest swelling was observed at pH 6.8 which evidences the possibility to release the drug in the colon. FT-IR and TGA confirmed carboxymethylation of tragacanth and the absence of drug-polymer interaction. The diclofenac sodium entrapment efficiency was 30–35% while the loading varies from 4.5 to 18% w/w based upon the drug-polymer ratio. The beads could extend the drug release up to 180 min at pH 6.8. The pH-responsive CM-TG hydrogel beads are biocompatible and could be exploited as a new excipient in developing enteric release formulations.

Formulation and Characterization of Atorvastatin Nanocystal Tablet

The aim of the present study was to investigate the effect of Soluplus on the solubility of atorvastatin and to develop a nanocrystals formulation that can improve the oral bioavailability of atorvastatin. We demonstrated that Soluplus increases the aqueous solubility of atorvastatin. Several nanocrystals formulations of atorvastatin with Soluplus were prepared at using drug: carrier ratio of 1: 1, 1: 1.1, 1: 1.2, 1: 1.3, 1: 1.4, 1: 1.5, 1: 1.6, 1: 1.7, 1: 1.8, 1: 1.9 and 1: 2 by anti-solvent precipitation. Physicochemical analysis demonstrated that atorvastatin is crystalline in each nanocrystals and the 1: 1 drug: carrier ratio provided the highest degree of sustained atorvastatin super saturation. The prepared nanocrystals were characterized by Fourier Transform Infrared Spectroscopy, Differential Scanning Calorimeter, X-ray Diffraction Study, Zeta potential Nuclear magnetic resonance and Scanning Electron Microscopy. Solubility and dissolution study was performed to check the enhanced properties of nanocrystals of atorvastatin. It was observed that, nanocrystals tablet containing nanocrystals exhibited significantly faster solubility and drug dissolution as compared with conventional and marketed tablet of a drug. Amongst all nanocrystals formulations with drug polymer ratio 1: 1 shows highest solubility that is 2.5027±0.77 as compared to pure drug 0.4918±0.51 mg/ml. This increase solubility and dissolution due to increased surface area and characteristics of nanocrystals and soluplus.

Studying the Effect of Variables on Acyclovir Microsponge

The aim of the present investigation was to develop a microsponge delivery system of acyclovir to control its release when applied topically thereby reducing dosing frequency and enhancement patient compliance. The microsponges were produced by the oil in oil emulsion solvent diffusion method. The effect of different formulation and process variables such as internal phase volume, polymer type, drug-polymer ratio, stirring speed and stirring duration on microsponge production yield, loading efficiency, particle size and in-vitro drug release was evaluated. The result showed that the microsponge F2 prepared from Eudrajet RS polymer had optimum physical properties regarding the loading efficiency of 99.71_+ 0.7% and production yield which was 85%. Also, F2 showed 66% drug release within 8 hours. Accordingly, the oil in oil emulsion solvent diffusion method is an effective technique to formulate microsponges with maximum production yield and loading efficiency for acyclovir.

Development and optimization of orodispersible tablets using solid dispersion of Telmisartan

The present study aimed towards the development of active delivery system for management of hypertension. The Orodispersible tablets (ODTs) containing Telmisartan was developed in order to accomplish enhanced solubility leading to better bioavailability profile. Different ratios, of Telmisartan and PEG 6000 i.e. 1:1, 1:2, 1:3, 1:4 and 1:5 were selected for the formulation of ODT system. A batch process was adopted for the preparation of solid dispersion with each combination of drug and polymer and the finally compressed as tablets by direct compression technique. For the preformulation perspective materials were scrutinized on the basis of solubility profile, drug content, Fourier Transform Infrared (FTIR) spectroscopy and Differential scanning calorimetry (DSC). The drug polymer ratio 1:4 was selected for further compression process. The prepared batches of ODTs were characterized for micromeritic study, thickness, hardness, weight variation, wetting time, disintegration time, drug content and in vitro drug release profile. The evaluation data for all batches was satisfactory out of them formulation TF3 containing 6% kyron T-314 showed the best results with a value of 29.3 sec and 24.1 sec for wetting and disintegration, respectively. This formulation showed superior drug release of 99.93% over a period of 30 minutes.

Antibiotic evaluation of odontogenic microbiological spectrum of orofacial infection

The present study aimed towards the development of active delivery system for management of hypertension. The Orodispersible tablets (ODTs) containing Telmisartan was developed in order to accomplish enhanced solubility leading to better bioavailability profile. Different ratios, of Telmisartan and PEG 6000 i.e. 1:1, 1:2, 1:3, 1:4 and 1:5 were selected for the formulation of ODT system. A batch process was adopted for the preparation of solid dispersion with each combination of drug and polymer and the finally compressed as tablets by direct compression technique. For the preformulation perspective materials were scrutinized on the basis of solubility profile, drug content, Fourier Transform Infrared (FTIR) spectroscopy and Differential scanning calorimetry (DSC). The drug polymer ratio 1:4 was selected for further compression process. The prepared batches of ODTs were characterized for micromeritic study, thickness, hardness, weight variation, wetting time, disintegration time, drug content and in vitro drug release profile. The evaluation data for all batches was satisfactory out of them formulation TF3 containing 6% kyron T-314 showed the best results with a value of 29.3 sec and 24.1 sec for wetting and disintegration, respectively. This formulation showed superior drug release of 99.93% over a period of 30 minutes.
 Keywords: Telmisartan, PEG 6000, Angioten receptor-II antagonist, Solid dispersion, Kyron T-314

Spray dried solid dispersions of piroxicam in carboxymethyl sago cellulose using aqueous solvents: A simple, novel and green approach to produce enteric microparticles with enhanced dissolution

Piroxicam-CMSC solid dispersions were produced by spray drying from aqueous solvents. Depending on the drug-polymer ratio, loading and entrapment efficiency of CMSC microparticles were 6.8–46.75 and 40.79–60.35% w/w, respectively. Scanning electron microscopy revealed non-spherical geometry and agglomeration of the spray-dried particles. The average size of the particles ranged from 7 to 170 µm. Infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction confirmed intact crystalline piroxicam in the microparticles. In gastric pH, microparticles and native piroxicam have shown less than 25% and more than 45% of drug dissolution, respectively in 2 h. In contrast, at pH 7.4, microparticles have shown 80% of drug dissolution; whereas native piroxicam achieved only 30% of dissolution by 30 min. The spray-dried CMSC particles are efficient in restricting drug release in gastric pH and enhance drug dissolution in intestinal pH. The method is eco-friendly as it uses aqueous solvents and non-toxic materials.

FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods: Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine formulations were formulated and evaluated for possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate.
 Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

ENHANCEMENT OF THE SOLUBILITY AND THE DISSOLUTION RATE OF CANDESARTAN CILEXETIL USING MICROSPONGE TECHNOLOGY

Objective: The aim of the present study is to enhance the dissolution rate of candesartan cilexetil (CC) using microsponges. Candesartan is therapeutically a potent antihypertensive agent, but it suffers a major drawback of poor oral bioavailability, which is estimated to be 15% due to its low solubility in the gastrointestinal fluids and hepatic first-pass metabolism.Methods: Eudragit-based microsponges were prepared by quasi-emulsion solvent diffusion method using different drug–polymer ratios (1:1 to 1:6), stirring speeds (250–750 rpm), and emulsifier concentrations (polyvinyl alcohol) (0.05%–0.083% w/v). Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) study for CC, physical mixtures of drug–polymer, and selected formula were investigated to estimate compatibility of CC with other used ingredients. All formulations were evaluated for particle size, production yield, and loading efficiency. The in vitro drug release study of optimized formulation was performed in phosphate buffer pH 6.8.Results: The obtained results indicated that formula F3 which contains eudragit RS100 at drug:polymer ratio (6:1) was showed the smallest particle size with higher production yield and loading efficiency. DSC and FTIR study of the physical mixtures of drug and polymer revealed no drug–polymer interaction. The results clearly confirm that the percentage of CC released at 30 min from F3, CC powder, and self-made tablet was 54%, 20.325, and 38.9%, respectively.Conclusion: Microsponges technique was considered as a promising system to enhance the solubility and dissolution rate of poor-water soluble CC.

Influence of drug-polymer ratio on physical characteristics and release of metformin hydrochloride from metforminalginate microspheres

Purpose: To investigate the effect of drug and polymer ratio on the physical characteristics and release rate of metformin hydrochloride from alginate microspheres. Methods: Microspheres were prepared by ionotropic gelation aerosolization technique using sodium alginate as polymer and calcium chloride as crosslinker. Three formulations of drug and alginate polymer ratios: 1:1 (F1); 1:1.5 (F2); and 1:2 (F3), and 10 % calcium chloride (CaCl2) were investigated. The microspheres were studied with respect to physical characteristics, release profile and release rate. Release evaluation was done at pH 1.2 in hydrochloric acid (HCl) for 2 h, and in phosphate-buffered saline (PBS) at pH 7.4 for 12 h. Results: Drug loading in formulations F1, F2 and F3 were 3.08 ± 0.21, 3.34 ± 0.28, and 3.99 ± 0.19 %, respectively. Low entrapment of below 15 % was achieved for all formulations, whereas high yield (above 45 %) was obtained. Drug release above 74 % was observed for all formulations. The release rates of F1, F2 and F3 were 9.6390 x 10-2, 9.0985 x 10-2 , and 8.3312 x 10-2 %/min, respectively. Conclusion: Metformin-alginate microspheres can be used for optimized formulations with good physical characteristics and in vitro release. These findings suggest that the microspheres might be a potent drug delivery system for the treatment of diabetic mellitus.

Effective sustained release of 5-FU-loaded PLGA implant for improving therapeutic index of 5-FU in colon tumor

In this study, a biodegradable implant composed of poly(lactide co-glycolide) (PLGA) and 5-fluorouracil (5-FU) was fabricated by mold method and used to impede the colon cancer via the local sustained release of 5-FU after transplanting into the peritoneal cavity. To optimize the 5-FU-implant, different factors such type of polymer, polymer-drug ratio, hydrophilic additives and organic solvents were investigated based on in vitro 5-FU release behavior. The optimized 5-FU-implant was subjected to evaluate the capacity of sustained release of 5-FU in vitro and in vivo. In addition, the pharmacokinetics and bio-distribution of 5-FU-implant were also tested in vivo after grafting into the peritoneal cavity in rat. Moreover, different doses of 5-FU-implants were compared against 5-FU injection for their antitumor activity in colon cancer model in nude mice and for their safety in health rat. The results revealed that the optimized 5-FU-implant possessed excellent sustained release of 5-FU for 2 week and no burst release were observed in vitro and in vivo. The pharmacokinetic behavior showed that higher concentration of 5-FU was found in peritoneal fluid when compared to plasma, which resulted in significantly improving antitumor activity as well as decreasing the side effect. It was proved that the 5-FU-implant was more efficacious and much safer than 5-FU bolus injection, which would be also used to overcome the reoccurrence of colon cancer after surgery.

Preparation and evaluation of dual modified Godare (<i> Colocasia esculenta</i>) starch as a sustained release excipient in tablet formulations

Starch obtained from Colocasia esculenta, Araceae (locally known as godare) has been pregelatinized, cross-linked and evaluated as a sustained release excipient and hydrophilic matrix former in tablet formulations. The pregelatinized starch (PGS) was cross-linked in a microwave oven at three different powers (90, 220 and 350 W) and reaction times ranging from 1 to 6 min, using sodium hexametaphosphate (SHMP) as cross-linking agent. Theophylline tablets containing 30, 40, and 50% and the modified starches were compressed at a constant compression force. Dissolution profiles of theophylline were determined in 0.1 N HCl for the first 2 h and then in phosphate buffer pH 6.8 for the remaining 10 h. Degree of cross-linking (DC) increased with increasing reaction power and time. The resulting modified starches were found to be freely flowing, moisture and acid resistant. Two of the nine theophylline tablet formulations sustained the release over the study period of 12 h releasing about 90% of the drug. The in vitro drug release showed best fit to Higuchi and Hixson-Crowell models depending on the polymer-drug ratio and the type of matrix formers. The dual modified starch in a concentration ranging from 40 to 50% exhibited the attributes of sustained release matrix-forming polymer in the tablet formulations studied. Keywords: godare starch, dual modification, microwave, sustained release, hydrophilic matrix

PREPARATION AND EVALUATION OF DROTAVERINE HCL ORAL DISINTEGRATING TABLETS USING SOLID MIXTURE TECHNIQUE

Objective: The objective of this study is to formulate orally disintegrating taste masked tablets of drotaverine HCl using solid mixture technique.Methods: Taste masked drug-polymer solid mixtures of drotaverine HCl were prepared by using hydroxypropyl methylcellulose (HPMC) 3 cps and rxcipient® FM1000/calcium silicate (rxcipient) as carriers employing kneading method using varying drug-polymer ratios of 1:1, 1:5, 1:7.5, and 1:9. Prepared drug-polymer mixtures evaluated for taste masking, and the ratio of drug-polymer is optimized. The granules and tablets prepared with optimized drug-polymer ratio were evaluated for pre- and post-compression parameters, in vitro dissolution studies, Fourier-transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD) studies.Results: The drug:polymer ratios 1:7.5 with rxcipient and 1:9 with HPMC were optimized based on taste evaluation. The pre-compression results showed that all the formulae have good flow properties. The post-compression evaluations showed that all the formulae met the specifications of orally disintegrating tablets. From all the prepared taste masked drotaverine HCl tablets, R10 formulation consisting of 4% croscarmellose sodium and H9 formulation consisting of 3% croscarmellose sodium, 3% sodium starch glycolate, and 2% microcrystalline cellulose shown more than 99% drug release in 60 min, and both the formulations showed better taste masking and were meting oral disintegrating tablet (ODT) parameters. The optimized formulation was characterized by FTIR, DSC, and XRD studies and found no incompatibility.Conclusion: The results demonstrated that the prepared drotaverine HCl ODT showed better taste masking and meeting the parameters of ODT formulations R10 and H9. The present solid mixture technique can be effectively used for taste masking.

PREPARATION, CHARACTERISATION AND EVALUATION OF ROPINIROLE HYDROCHLORIDE LOADED CONTROLLED RELEASE MICROSPHERES USING SOLVENT EVAPORATION TECHNIQUE

Objective: The major objective of the research work was to design, characterise and evaluate controlled release microspheres of ropinirole hydrochloride by using non-aqueous solvent evaporation technique to facilitate the delivery of the drug at a predetermined rate for a specific period of time.Methods: Ropinirole hydrochloride microspheres were prepared by using different low-density polymers such as eudragit RL 100, eudragit RS 100 and ethylcellulose either alone or in combination with the help of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as particle size analysis, micrometric properties, drug entrapment efficiency, percentage drug loading, percentage yield and in vitro drug release study. The compatibility of the drug and polymers was confirmed by physical compatibility study, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and x-ray diffraction study (XRD). The formation of the most optimized batch of the microsphere (F12) was confirmed by scanning electron microscopy (SEM), DSC, FTIR, and XRD. In vitro drug release study and in vitro drug release kinetics study of the formulated microspheres were also carried out.Results: Drug-polymer compatibility studies performed with the help of FTIR and DSC indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique was a suitable technique for the preparation of microspheres as most of the formulations were discrete, free-flowing and spherical in shape with a good yield of 55.67% to 80.09%, percentage drug loading of 35.52% to 94.50% and percentage drug entrapment efficiency of 36.24% to 95.07%. Different drug-polymer ratios, as well as the combination of polymers, played a significant role in the variation of over-all characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, percentage drug loading, percentage drug entrapment, percentage yield, rheological studies and in vitro drug release characteristics, formulation F12 was found to fulfil the criteria of ideal controlled release drug delivery system. F12 showed controlled release till the 14th hour (97.99%) and its in vitro release kinetics was best explained by zero-order kinetics and followed Korsemeyer-Pappas model (Non-Fickian mechanism). SEM of F12 revealed the formation of spherical structures. The FTIR study of F12 confirmed the stable nature of ropinirole in the drug-loaded microspheres. DSC and XRD patterns showed that ropinirole hydrochloride was dispersed at the molecular level in the polymer matrix.Conclusion: The controlled release microparticles were successfully prepared and from this study, it was concluded that the developed microspheres of ropinirole hydrochloride can be used for controlled drug release to improve the bioavailability and patient compliance and to maintain a constant drug level in the blood target tissue by releasing the drug in zero order pattern.

Formulation and In Vitro Evaluation of Ciprofloxacin Matrix Tablets: Effect of Drug-Polymer Ratio

Formulation and In Vitro Evaluation of Ciprofloxacin Matrix Tablets: Effect of Drug-Polymer Ratio

FABRICATION AND EFFECT OF PROCESS VARIABLES OF SITAGLIPTIN MICROSPHERES

Objective: The study is to formulate and assess the effects of different variables on the release profile of sitagliptin microspheres.Methods: The microspheres were prepared by emulsion-solvent diffusion method and ionotropic gelation method using ethyl cellulose and sodium alginate as the polymers, respectively. The formulations are optimized by applying 23 factorial design based on the drug-polymer ratio, stirring speed, and method of preparation.Results: The drug-polymer interaction was checked by the Fourier-transform infrared spectroscopy and differential scanning calorimetry the results of which indicated no incompatibility. The formulated sitagliptin microspheres were evaluated for shape, morphology, particle size, the degree of swelling, encapsulation efficiency, in vitro drug release studies for 12 h, and kinetics of drug release.Conclusion: The results showed that the drug-polymer ratio and stirring speed affected the particle size and drug release. The release of the drug was found to be sustained, and diffusion path is following cube root law of Hixson-Crowell kinetics. The batch F3 was found to be desirable and was further characterized by scanning electron microscope for morphology.

DEVELOPMENT AND IN VITRO EVALUATION OF AN ORAL FLOATING TABLET OF METRONIDAZOLE

The present study was undertaken with an aim to develop and evaluate gastroretentive floating tablets of Metronidazole that are designed to retain in the stomach for a long time and have developed as a drug delivery system for better eradication of Helicobacter Pylori in peptic ulcer diseases. The floating tablets of Metronidazole were made by direct compression method using polymer Carbopol 934 and sodium bicarbonate and citric acid as gas generating agent. The tablets were evaluated by pre and post compression parameters such as weight variation, thickness, friability, hardness, drug content, in- vitro buoyancy studies and in-vitro dissolution studies and results were within the limits. Hardness was found to be in the range of 7.6 ± 0.27 kg/ cm² to 7.9 ± 0.35 kg/cm², the percent friability was in the range of 0.48% to 0.52% w/w and the tablets showed 94% to 97% uniformity in drug content. The in-vitro dissolution studies were carried out in a USP type- II apparatus in 0.1N HCl. The formulations were able to within 2-7 minutes and showed buoyancy >12 hrs. The drug-polymer ratio, viscosity grades of Carbopol 934 and gas generating agents were found to influence the release of drug and floating characteristics from the prepared floating drug delivery system of Metronidazole. Kinetically, among the 4 assessed models the release pattern of Metronidazole from the tablets fitted best to Higuchi’s and zero order indicated that diffusion is the predominant mechanism controlling the drug release. Keywords: Metronidazole, Floating tablets, Carbopol 934, Gastroretentive, Dissolution

Sustain Release Microsponge Based Drug Delivery System for the Plasmodium Treatment: Formulation Development and In vitro - In vivo Evaluation

The aim behind the present research work was to develop a microsponge based dosage form for sustained delivery of Artemether prepared by quasi-emulsion solvent diffusion method using polymer Eudragit RS-100 with two factors drug-polymer ratios and rate of agitation for optimization purposes, these two factors influences micro particles and physical properties. Sophisticated characterization techniques followed for the formed microsponges were DSC, FT-IR, SEM and particle size analysis, along with morphology, drug loading and in-vivo - in-vitro drug release data, DSC and FT-IR data reveals that there were no chemical interactions between drug Artemether and polymers Eudragit RS-100 used. The drug-polymer ratio and rate of agitation showed remarkable impact on drug content, encapsulation efficiency and particle size, SEM micrographs revealed that microsponges formed were spherical in shape with porous surface, and had 21.2591 ± 0.08 μm mean particle size. The microsponges were then loaded in capsules followed by in-vitro drug release study; which depicted that microsponges with drug-polymer ratio of 1:5 at 500 rpm were more proficient to give extended drug release of 96.46 ± 0.06 % at the end of 12 h, better in contrast to conventional market formulation. Hence, the developed microsponge based formulation of Artemether would be an expectant, promising substitute to conventional therapy for the Plasmodium treatment.

Surface area normalized dissolution to study differences in itraconazole-copovidone solid dispersions prepared by spray-drying and hot melt extrusion

Amorphous solid dispersions of itraconazole (ITZ) and copovidone (PVPVA 64) at 1:1 to 1:9 drug-polymer ratios were prepared using spray-drying (SD) and hot melt (HM) extrusion for comparative evaluation. Surface area normalized dissolution studies were carried out using a modified intrinsic dissolution rate (IDR) assembly and rate of release of drug as well as polymer were quantified using ultraviolet spectroscopy. The melt quenched amorphous form of ITZ provided an 18-fold dissolution advantage over the crystalline form. In general, dispersions prepared by either SD or HM showed similar dissolution profiles in terms of drug release. Both drug-controlled and polymer-controlled ITZ dissolution rates were observed, depending on the drug loading, where a switch from a drug-controlled to a polymer-controlled regime was observed when the drug loading was approximately 20% or lower. The impact of the spray drying solvent composition was studied and found to have a large effect on the drug release rate for dispersions containing a drug loading of 20%. Electron microscopy showed differences in surface morphology (scanning) and internal structure (transmission) in these dispersions as a function of solvent system. X-ray photoelectron spectroscopy (XPS) revealed differences in the surface composition of drug and polymer whereby poorly dissolving systems showed drug enrichment. This study provides insight into the complex interplay between formulation, processing and performance of amorphous solid dispersion systems.

Development and Evaluation of Terbinafine Hydrochloride Polymeric Microsponges for Topical Drug Delivery

The objective of the present study was to develop and evaluate sustained delivery of terbinafine hydrochloride from topical polymeric microsponges. Microsponges of ethyl cellulose containing terbinafine hydrochloride were prepared by quasi emulsion solvent diffusion method. Effect of drug polymer ratio on active drug content, particle size and entrapment efficiency were studied. Drug polymer ratio greatly affects properties (entrapment efficiency, active drug content, particle size) of microsponges. Terbinafine hydrochloride microsponges showed highest actual drug content, entrapment efficiency and smaller particle size, so 1.5:1 ratio of drug and polymer was selected for optimization study. Optimization study was carried out by taking internal phase volume, stirring rate, emulsifier concentration as independent variables and their effects on entrapment efficiency, particle size were studied. It was found that as stirring speed increases, the particle size decreases and entrapment efficiency increases, while as volume of dichloromethane increases, particle size decreases. Morphology of obtained microsponges was revealed by scanning electron microscope and was found to be porous and spherical. Optimized formulation of microsponge was dispersed in Carbopol gel and evaluated for drug content, pH, viscosity and in vitro drug release. Release of drug was found to be sustained through microsponge gel as compared to marketed product and pure drug gel. Ex vivo drug deposition study was carried using rat abdominal skin. Drug deposition was found to be satisfactory. Prepared polymeric microsponges could be a potential topical drug delivery system in antifungal therapy.

Preparation and Characterization of Paracetamol Loaded Eudragit S100 Nanoparticles by Salting Out Technique

The aim of this study was to prepare Paracetamol loaded Eudragit S100 nanoparticles by salting out (SO) technique. Eudragit S100 (ED) was used as a polymer. Paracetamol and polymer were dissolved in ethanol at various drug-polymer ratios (1:1, 1:2 and 1:3), among three formulations 1:3 was found to be the best formulation with drug content of 80.3% and entrapment efficiency was found to be 99.8%. Loading capacity was found to be more for 1:3 formulation. Na.cmc was used as stabilizer and ZnSO4.7H2O was used as a salting out agent and ethanol were used as solvent.