Invitro Drug Release Studies Research Articles

QBD approach for green synthesis of Rutin silver nanoparticles- screening for antioxidant, anticancer and anticlastogenic potential

Rutin is a flavonoid glycoside abundant in many plants exhibiting pharmacological activities like antioxidant, anticancer, anti-inflammatory and antimicrobial activities. Plant biomarkers suffer low bioavailability and solubility that lack clinical effectiveness. The smart nanoparticles conversion addresses this limitation with optimal particle size and targeted drug delivery. The present study involves QbD approach for formulation of Rutin silver nanoparticles and evaluation of antioxidant, anticancer and anticlastogenic potential. QbD experimentation involved particle size and drug release as dependent variables over the silver nitrate concentration, methanol and sonication time as independent variables devising 15 formulations (F1 –F15). F12 formulation was found to be optimized with 126.3 nm average size, stable and dispersible characterized by UV, FTIR, SEM and DLS studies. The calibration curve of Rutin was plotted at 352 nm with linearity (LOD = 0.061 μg/ml and LOQ = 0.187 μg/ml). The invitro drug release studies by USP dissolution apparatus I (Basket type) proved the sustained release characteristics with 97.3 % drug release when compared to the Rutin. The pharmacological screening for potential antioxidant and anticancer activity on G361 and MCF 7 cell line of F12 formulation have shown promising results and also enhanced solubility in water compared to Rutin. Anticalstogenic potential as a function of induced micronuclei frequency was evaluated as a characteristic feature in bone marrow cells obtained from mice. Results indicate pre-treatment with the F12 reduced frequency of micronuclei in mouse bone marrow cells caused by Cyclophosphamide (CP) significantly. The protective effect of F12 in suppression was demonstrated at both dosages of 100 and 200 mg/kg. Thus the findings suggest the novel Rutin silver nanoparticles as lead drug serving as antioxidant, anticancer and anticlastogenic agent.

Development and characterization of ferulic acid-loaded chitosan nanoparticle embedded- hydrogel for diabetic wound delivery

Diabetic wounds present a significant global health challenge exacerbated by chronic hyperglycemia-induced oxidative stress, impeding the natural healing process. Despite various treatment strategies, diabetic foot ulceration lacks standardized therapy. Ferulic acid (FA), known for its potent antidiabetic and antioxidant properties, holds promise for diabetic wound management. However, oral administration of FA faces limitations due to rapid oxidation, stability issues, and low bioavailability. The topical application of FA-loaded chitosan nanoparticles (FA-CSNPs) has emerged as a promising approach to overcome these challenges. Here, we report the development of a sustained-release formulation of FA-CSNPs within a hydrogel matrix composed of Chitosan and gelatin. The FA-CSNPs were synthesized using the ionic gelation method andoptimized through a Central Composite Design (CCD) approach. Characterization of the optimized nanoparticles revealed spherical morphology, a particle size of 56.9 ± 2.5 nm, and an impressive entrapment efficiency of 90.3 ± 2.4 %. Subsequently, an FA-CSNPs-loaded hydrogel was formulated, incorporating chitosan as a gelling agent, gelatin to enhance mechanical properties and cell permeation, and glutaraldehyde as a cross-linker. Comprehensive characterization of the hydrogel included pH, moisture loss, porosity, swelling index, rheology, water vapor transmission rate (WVTR), SEM, TEM, invitro drug release studies, antioxidant activity, antibacterial efficacy, cell cytotoxicity, cell migration studies on L929 fibroblast cell line, and stability studies. The stability study demonstrated negligible variations in particle size, zeta potential, and entrapment efficiency over 60 days, ensuring the stable nature of nanoparticles and hydrogel. This innovative delivery approach embedded within a hydrogel matrix holds significant promise for enhancing the therapeutic efficacy of FA-CSNPs-hydrogel in diabetic wound healing applications.

Formulation and Evaluation of Taste Masked Chewable Tablet containing Curcumin, Acetaminophen, and Ascorbic acid to treat sore throat

Objective: This study was intended to investigate the formulation and characterization of Mesalamine or 5-Aminosalicylic acid (5-ASA) pellets using novel excipient and formulated as matrix spheres to controlled the drug release extended period of time. Uniformly distributed throughout the gastrointestinal tract and Avoid dose dumping of drug. Methods: Mesalamine's active pharmaceutical component was characterised, and investigations were conducted prior to formulation to ensure a physical combination of the drug and excipients was achieved. Formulation of mesalamine as matrix pellets by using fluid bed processor and mesalamine loaded into seal coated sugar spheres and extended-release coating with Ethyl cellulose. Ethyl cellulose is pH independent polymer and retarder the drug release throughout the gastrointestinal tract and site-specific action in colon. Hypromellose also act as pore former and drug release based on diffusion mechanism. In drug layering, core pellets contain stearic acid and hydrogenated castor oil internally forming a matrix. Developed mesalamine pellets are characterized such as drug content, invitro drug release and appearances and particle size distribution. Results: Development of Mesalamine pellets based on five strategy From MEZ 1 to MEZ 5 are formulated and Characterization are performed. Based on the invitro drug release studies, we concluded that the formulation MEZ-IV was best formulation. Invitro drug release is consistence throughout 12hours.(1hrs-23%, 2nd hrs 41%, 4hrs-73, 6hrs-86, 8hrs-99% and 12hrs-10.

Levofloxacin loaded chitosan and poly-lactic-co-glycolic acid nano-particles against resistant bacteria: Synthesis, characterization and antibacterial activity

BackgroundWith the global increase in antibacterial resistance, the challenge faced by developing countries is to utilize the available antibiotics, alone or in combination, against resistant bacterial strains. We aimed to encapsulate the levofloxacin (LVX) into polymeric nanoparticles using biodegradable polymers i.e. Chitosan and PLGA, estimating their physicochemical characteristics followed by functional assessment as nanocarriers of levofloxacin against the different resistant strains of bacteria isolated from biological samples collected from tertiary care hospital in Lahore, Pakistan. MethodsLVX-NPs were synthesized using ion gelation and double emulsion solvent-evaporation method employing chitosan (CS) and poly-lactic-co-glycolic acid (PLGA), characterized via FTIR, XRD, SEM, and invitro drug release studies, while antibacterial activity was assessed using Kirby-Bauer disc-diffusion method. ResultsData revealed that the levofloxacin-loaded chitosan nanoparticles showed entrapment efficiency of 57.14% ± 0.03 (CS-I), 77.30% ± 0.08(CS-II) and 87.47% ± 0.08 (CS-III). The drug content, particle size, and polydispersity index of CS-I were 52.22% ± 0.2, 559 nm ± 31 nm, and 0.030, respectively, whereas it was 66.86% ± 0.17, 595 nm ± 52.3 nm and 0.057, respectively for CS-II and 82.65% ± 0.36, 758 nm ± 24 nm and 0.1, respectively for CS-III. The PLGA-levofloxacin nanoparticles showed an entrapment efficiency of 42.80% ± 0.4 (PLGA I) and 23.80% ± 0.4 (PLGA II). The drug content, particle size and polydispersity index of PLGA-I were 86% ± 0.21, 92 nm ± 10 nm, and 0.058, respectively, whereas it was 52.41% ± 0.45, 313 nm ± 32 nm and 0.076, respectively for PLGA-II. The XRD patterns of both polymeric nanoparticles showed an amorphous nature. SEM analysis reflects the circular-shaped agglomerated nanoparticles with PLGA polymer and dense spherical nanoparticles with chitosan polymer. The in-vitro release profile of PLGA-I nanoparticles showed a sustained release of 82% in 120 h and it was 58.40% for CS-III. Both types of polymeric nanoparticles were found to be stable for up to 6 months without losing any major drug content. Among the selected formulations, CS-III and PLGA-I, CS-III had better antibacterial potency against gram+ve and gram-ve bacteria, except for K. pneumonia, yet, PLGA-I demonstrated efficacy against K. pneumonia as per CSLI guidelines. All formulations did not exhibit any signs of hemotoxicity, nonetheless, the CS-NPs tend to bind on the surface of RBCs. ConclusionThese data suggested that available antibiotics can effectively be utilized as nano-antibiotics against resistant bacterial strains, causing severe infections, for improved antibiotic sensitivity without compromising patient safety.

Design, Evaluation and Optimization of Albuterol Sulphate and Theophylline Pulsincap drug delivery system for chronotherapy of Asthma

The aim of the current study was to design and develop and evaluate pulsatile drug delivery system of Albuterol Sulphate and Theophylline for the treatment of Asthma. The capsule body was made water insoluble by cross linked with formaldehyde vaopur. The treatment of Formalin was adopted to modify the gelatin capsule solubility. The formalin residue was carried out by quantitative test. The drug-excipient compatibility is done by FTIR and UV . The pulsincap formulation were prepared by using hydrogel plug of various components. The drug content of the formulation of pulsincap was found to be in the general range. The invitro drug release studies in ph1.2 .6.2 and 7.4 buffern was noticed to be zero percent and capsule was stable for 2 hours drug the studyF5 formulation batch was selected which was best and good formulation and promoted maximum drug release of 96.29% percentage at phosphate buffers when compared with other formulation. Pulsincap formulation can be adopted for optimum delivery of pellets in the treatment as per chronotherapy
 Keywords: Theophylline, quantitative test, invitro drug release studies, phosphate buffers6.2 and 7.4.

Fabrication of dual drug-loaded polycaprolactone-gelatin composite nanofibers for full thickness diabetic wound healing.

Aim: Design of moxifloxacin and ornidazole co-loaded polycaprolactone and gelatin nanofiber dressing for diabetic wounds. Materials & methods: The composite nanofibers were prepared using electrospinning technique and characterized for in vitro drug release, antibacterial activity, laser doppler and in vivo wound healing. Results: The optimized nanofiber demonstrated an interconnected bead free nanofiber with average diameter <200nm. The invitro drug release & antimicrobial studies revealed that optimized nanofiber provided drug release for >120h, thereby inhibiting growth of Escherichiacoli and Stapyhlococcusaureus. An in vivo wound closure study on diabetic rats found that optimized nanofiber group had a significantly higher wound closure rate than marketed formulation. Conclusion: The nanofiber provided prolonged drug release and accelerated wound healing, making it a promising candidate for diabetic wound care.

Innovative Nanosuspension Formulation for Prochlorperazine and In-vitro Evaluation

Prochlorperazine is a dopamine antagonist and is used to control nausea and vomiting. It is a BCS class II drug which has low aqueous solubility and high permeability. The present study is aimed to formulate and evaluate prochlorperazine nanosuspension to improve solubility and enhance dissolution of Prochlorperazine with varying concentrations of stabilizers such as Tween 80, PVP K30, Poloxamer 188 by using nanoprecipitation method. The developed formulations were characterized for particle size and polydispersity index, total drug content, SEM, Zeta Potential and FTIR. The invitro drug release studies and invitro drug release kinetics were performed for all formulations. FTIR studies revealed that drug is compatible with the excipients. The particle size and poly dispersity index of optimized formulation was found to be 162nm and the zeta potential was found to be -30.2 mV and concluded that the system had sufficient stability. The invitro drug release was found within their acceptable ranges. The rate of dissolution of best batch was enhanced to 93.24 in 120min. Stability studies proved that nanosuspensions were more stable with no significant changes in particle size distribution. Thus the formulated nanosuspension of prochlorperazine offers a superior conventional dosage forms for drug release&#x0D; Keywords: Prochlorperazine, Nanosuspension, Solubility, Dissolution

Formulation of Methotrexate Loaded Solid Lipid Nanoparticles By Micro Emulsion Technique

AIM: The aim of this study was to develop and characterize Methotrexate loaded solid lipid nanoparticles by Microemulsion technique. Background: Methotrexate is a preferable anti metabolite drug. It is used in the treatment of certain cancers like breast cancer, skin and lung cancer. Clinical studies have revealed that the curative effect of MTX tablet on cancers was limited due to their toxic dose-related side effects to normal cells, nephrotoxicity, and bone marrow suppression, acute and chronic hepatotoxicity and also due to the drug resistance of the tumour cells. Hence, there is a need to develop methotrexate solid lipid nanoparticles in order to minimize the adverse effects associated with the MTX tablet dosage form. Objective: The objective of the research work is to formulate, characterize and evaluate Methotrexate solid lipid nanoparticles by micro emulsification solidification technique. Methods: Solid lipid nanoparticles are prepared by using lipids stearic acid and glycerol monostearate by varying the concentration of surfactant. Three formulations were prepared with each lipid. Micro emulsion technique was adopted for the preparation of solid lipid nanoparticles. Each formulation was evaluated for drug content, entrapment efficiency, loading capacity&amp; invitro drug release studies. Both the lipids were compared for the characterization and evaluation parameters. Result: On comparison Glycerol monostearate was found to be a better lipid over Stearic acid for the preparation of Methotrexate solid lipid nanoparticles because of its smaller mean particle diameter (238.8 nm), higher stability (-56.5 mV) and greater entrapment efficiency. Conclusion: Methotrexate solid lipid nanoparticles were successfully prepared with higher stability and drug release rate.

FORMULATION AND EVALUATION OF TRAMADOL HYDROCHLORIDE LOADED TRANSFEROSOMAL GEL BY THIN FILM HYDRATION TECHNIQUE

Objective(s): The current studys goal is to develop and test a tramadol hydrochloride transdermal gel based on vesicular drug delivery approaches. Materials and methods: Transferosomes were chosen as the colloidal carrier for tramadol hydrochloride transdermal gel preparation. Thin film hydration was used to create transferosomes. The obtained transferosomes were characterised for drug content, vesicular diameter, zeta potential, entrapment efficiency, invitro drug release studies. Results: T5 (made via thin film hydration and comprising a soya lecithin: Tween 60 ratio of 1:2.5) was deemed the best transferosome formulation due to its 274.2nm mean vesicular diameter, -29.5 mV zeta potential, 93.9% drug content, 97% entrapment efficiency, and 92.7% sustained drug release after 12 hours. The T5 formulation was included into the gel. There was a comparison between plain gel and transfersomal gel. Transfersomal gel was rated superior to the other gels due to its higher drug concentration (91%), spreadability (18.35 g.cm/sec), pH (6.9), and sustained drug release profile over 12 hours. Conclusion: By comparing transferosomal gel with plain gel transferosomal gel indicated better results than plain gel.

Development of nanosilver embedded injectable liquid crystalline hydrogel from alginate and chitosan for potent antibacterial and anticancer applications

Injectable hydrogels with macroscopic ordering have gained special attention in drug delivery due to their excellent biocompatibility and minimally invasive surgical procedure. Nanosilver embedded Schiff base hydrogel from biopolymers alginate and chitosan was developed and demonstrated its application in the injectable delivery of anticancer drug Dox.HCl. The ordered hydrogel structure was evidenced by FT-IR, DLS, XRD and Rheology. The self-assembled morphology of nanosilver- Schiff base hydrogels was studied by microscopic techniques such as SEM, TEM and AFM. The pH dependent anticancer activity of the hydrogel was demonstrated by invitro drug release studies at pH 5.5 and 86.56 % release was obtained for 100 mgL-1 of Dox.HCl loaded hydrogel at 72 hours. The antibacterial activity attained from nanosilver can be assessed by Agar well diffusion assay and minimum inhibitory concentration and minimum biocidal concentrations were determined as 62.5 μL/mL and 125 μL/mL, respectively. The invitro cell viability studies were done against skin cancer cell B16 by MTT assay which shows 34.82 % of toxicity towards B16 cancer cells and the cell death was further confirmed by Apoptosis assay and flow cytometry. The developed macroscopically ordered liquid crystalline hydrogel can be act as a versatile platform for injectable drug delivery system.

Formulation and Evaluation of Self-Micro Emulsifying Drug Delivery System (SMEDDS) of Ticagrelor

The present work mainly emphasized on the enhancement of solubility of Ticagrelor by developing Self- Micro emulsifying drug delivery system. Ticagrelor is a BCS class IV drug with poor aqueous solubility and permeability. The saturated solubility of Ticagrelor in various oils, surfactants and co-surfactants was determined by using UV-spectroscopy. The excipients were selected based on their maximum solubility and compatibility for Ticagrelor. SMEDDS formulations od Ticagrelor were developed using different oils, surfactants and co-surfactant combinations (4:1 and 3:1). Pseudo ternary phase diagrams were constructed and based on pseudo ternary phase diagrams, Nano emulsification area was evaluated .Formulations were designed based on the pseudo ternary phase diagram using various proportions of oil (Capmul MCM E8 EP), surfactant (Labrasol), co-surfactant (PEG-400). The prepared formulations were selected among them F1 was optimized and carried out for further evaluations like dispersibility test, self-emulsification time ,phase separation and stability test, thermodynamic stability studies, droplet size and zeta potential, invitro drug release studies. The results of present study demonstrate that Ticagrelor SMEDDS can be used as a potential means for improving the solubility of Ticagrelor.

Formulation and Evaluation of Guaifenesin Gastro Retentive Tablets

Guaifenesin is an expectorant and belongs to BCS class I which exhibits high solubility and high permeability. Guaifenesin has a half-life of 1 hour; in order to increase its duration of action gastroretentive tablets are formulated. Guaifenesin shows poor flow properties so the method opted for the preparation of this tablets is Top spray granulation. In which HPMC K100LV/HPMC E6LV/HPMC K100M/HPMC K15MPCR is used as swelling matrix polymer, Povidone is used as binder, Magnesium stearate is used as lubricant and MCC is used as diluent. Tablets are evaluated for floating lag time, total floating time, thickness, hardness, friability and invitro drug release studies were performed. The optimized formulation showed less floating lag time, sufficient floating time and with maximum drug release of 88.9% at the end of 12 hours.

Lipid nanocarrier system of perinodopril for enhancement of bioavailability

Perinodopril comes under BCS class II drug (low solubility/high permeability) which shows variable absorption pattern due to solubility limitation. Therefore, nanostructured lipid carrier (NLC) of Perinodopril was developed which is suitable for drug with high log P value as it offers the advantage of high drug entrapment and loading capacity to lipophilic drugs. Tween 80 and Poloxamer 188 were reportedly P-gp efflux inhibitors which would be an added feature to the property of Perinodopril -NLC thus enhancing drug availability across intestine. So the objective of the current work was to evaluate the NLC of perinodopril formulation and to evaluate the same. The invivo estimation of the activity was carried out on Albino wistar rats that are maintained under room conditions and the formulation was investigated for the Pharamcokinetic and pharmacodynamic paramteres in rat plasma. Also they were tested for their stability invitro. Results show that the nano particles measured as 0.207nm in size. The invitro drug release studies suggest that the formulations were releasing the drug in controlled fashion during 23 hrs. Stability studies proves the drug is very stable in the formulation.

Evaluation and invitro gut permeation studies of solid lipid nano carrier mediated drug delivery system of perinodopril

High BP is one of the most predominant causes of heart diseases and cerebrovascular problems. Perinodopril is an ACE inhibitor that is a non sulfhydryl derivative that is used for the treatment of hypertension. To enhance the effect of the drug it was formulated into Lipid based nano carrier system (NLC) to improve the bioavailability and thereby the therapeutic potential. So the objective of the current work was to evaluate the NLC of perinodopril formulation and to evaluate the same. Animal protocol no. PCP/IACE/2019 and Registration no. 1678/PO/a/19/CPCS was approved by the Institutional Animal Ethics Committee (IAEC) at Pallavan Pharmacy College, Kanchipuram, Tamilnadu and their guidelines were followed. The invivo estimation of the activity was carried out on Albino wistar rats that are maintained under room conditions and the formulation was investigated for the Pharamcokinetic and pharmacodynamic paramteres in rat plasma. Also they were tested for their stability invitro. Results show that the nano particles measured as 0.207nm in size. The invitro drug release studies suggest that the formulations were releasing the drug in controlled fashion during 23 hrs.

Evaluation and invivo studies of solid lipid nano carrier mediated drug delivery system of perinodopril

High BP is one of the most predominant causes of heart diseases and cerebrovascular problems. Perinodopril is an ACE inhibitor that is a non sulfhydryl derivative that is used for the treatment of hypertension. To enhance the effect of the drug it was formulated into Lipid based nano carrier system (NLC) to improve the bioavailability and thereby the therapeutic potential. So the objective of the current work was to evaluate the NLC of perinodopril formulation and to evaluate the same. The invivo estimation of the activity was carried out on Albino wistar rats that are maintained under room conditions and the formulation was investigated for the Pharamcokinetic and pharmacodynamic paramteres in rat plasma. Also they were tested for their stability invitro. Results show that the nano particles measured as 0.207nm in size. The invitro drug release studies suggest that the formulations were releasing the drug in controlled fashion during 23 hrs. stability studies proves the drug is very stable in the formulation. With R2 = 0.9683, the in vitro-in vivo correlation research clearly shows good agreement between in vitro drug solubilization during lipolysis and in vivo drug absorption during pharmacokinetic studies.

Development of a Transdermal Delivery System for Tacrine

Tacrine has several mechanisms of action. The putative primary mechanism of action of tacrine for Alzheimer's disease is reversible inhibition of acetylcholinesterase (AChE), which thus slows the breakdown of the chemical messenger acetylcholine (ACh) in the brain. Tacrine also inhibits butyrylcholinesterase activity. In accumulation, tacrine blocks sodium and potassium channels. Tacrine also acts as a histamine N-methyltransferase inhibitor. This study was carried out to develop matrix based transdermal patches containing Tacrine to overcome the first pass metabolism and to reduce frequency of dosing compared to oral route. . Matrix type of transdermal patches was developed by using Methocel K4M, Methocel K15M, Methocel K100M and Xanthan gum polymers. Transdermal patches were prepared by employing solvent casting method. Drug excipients compatibility studies were carried out by using FTIR, and it was observed that there were no interactions. Formulations were prepared with the varying concentrations polymers ranging from F1-F16, and all the formulations were evaluated for various physical parameters Physical appearance, Flatness, Weight variation, Thickness, Folding endurance, Drug content, Moisture uptake, Moisture content and Swelling study and all the results were found to be within the pharmacopeial limits, invitro drug release studies by using dialysis membrane. Among all the 16 Tacrine transdermal patches formulations F5 formulations which contain Methocel K15M 100 mg had shown 97.61% % cumulative drug release within 12 hours.

Quality control and drug-drug interactions between commercially available Metoprolol and Glimepiride tablets

Quality is paramount and needs to be maintained throughout the shelf life of pharmaceuticals. The current study aimed to evaluate the quality, potency, and drug-drug interaction in an in vivo animal model by using two drugs, namely, metoprolol and glimepiride. Tablets were selected for their physical characteristics, such as shape, size, and color. Quality control tests, such as weight variation, hardness, friability, and disintegration tests, and invitro drug release studies were performed as per USP. Drug-drug interaction and in vivo studies were carried out according to the standard protocol of the animal ethics committee. Quality control tests of both the tablets were within the specified range. The cumulative release percentages of the drugs were 81.12% and 85.36% for Metoprolol Tartrate and Glimepiride, respectively, in a physiological buffer solution within 1 h. The combination of metoprolol and Glimepiride also significantly decreased the blood glucose level in diabetic animals. However, the blood glucose level increased in the group receiving metoprolol only, but the difference was not significant. The result suggested that the formulations are safe. However, the chronic use of this combination requires frequent monitoring of blood glucose level to improve its efficacy and for the patient’s safety.

Formulation and invitro evaluation of delayed release multiple unit pellets of Lansoprazole in capsules

The present research was aimed to formulate and evaluate Lansoprazole delayed release multiple unit pellets in capsules. Lansoprazole degrades in the acidic environment of the stomach. It is also unstable under conditions of high temperature and high humidity which leads to therapeutic inefficiency. Hence it is important to bypass the acidic pH of the stomach. Protection of drug from acidic environment is done by coating the drug with enteric polymer. In the present study, successive layers of drug layer, barrier layer and enteric layer was coated on the inert sugar spheres by using solution/suspension layering technique in Fluidized bed processor (FBP). The prepared drug layered and barrier layered pellets were evaluated for % yield. The prepared lubricated pellets were evaluated for flow properties i.e., bulk density, tapped density, compressibility index and hausner’s ratio. Lubricated pellets filled into size ‘1’ capsules and evaluated for drug content, drug content resisted in acid, invitro drug release studies and compared with the marketed product. The dissimilarity and similarity factors for the optimized and marketed formulations were found to be 84.29. Accelerated Stability Testing (AST) was performed as per the ICH guidelines at 40±5°C/75±5% RH for 6 months and found satisfactory.

Formulation and Evaluation of Mupirocin Nimosomal Gel for Topical Drug Delivery System

The present study was to formulate and evaluate the mupirocin niosomal gel using surfactants span 80 &amp; tween 80 for the preparation of niosomes. Mupirocin entrapped niosomes were prepared by ether injection method and transmembrane pH gradient drug uptake process. Niosomes were prepared by altering the ratios between various non-ionic surfactants (span 80 &amp; tween 80) whereas the concentration of cholesterol and drug was kept constant. The prepared niosomes were characterized for size, shape, entrapment efficiency, invitro drug release studies. The highest entrapment efficiency(99.17%) and drug release (96.14%) was obtained for tween 80 (1:5:5) prepared by transmembrane pH gradient method. The best formulation among the two techniques was selected for incorporated into gel formulation. The prepared niosomal gel and plain gel were subjected to evaluation studies like drug content, invitro drug diffusion studies. The studies were demonstrated that niosomal gel was shown beter pharmacological activity than the conventional mupirocin gel. Based on the results it was concluded that niosomal preparations offers more advantageous than the conventional preparations.

Formulation and Evaluation of Erythromycin Estolate Loaded Drug Balls

The purpose of research work was to develop and optimize drug balls of erythromycin estolate for oral mucosal delivery of drug for fast delivery of drug and better bio-availability with the aim to treatment of whooping cough with also additional advantages over the traditional dosage forms such as suspension and tablets which takes too much time for release of drug but drug balls release mucoadhesive liquid which shows fast drug release, better bioavailability, avoid hepatic first pass effect and fast action. Sodium alginate based drug balls containing erythromycin estolate were prepared by specific method. Sodium alginate, ethyl cellulose were selected on the basis of formulation of drug balls, mucoadhesive force, In-vitro drug release. A 32 factorial design was employed for preparation of drug balls wherein the concentration of sodium alginate, concentration of ethyl cellulose were selected as independent variables while in vitro drug release and percentage permeation were the dependent variables. Drug balls were evaluated with respect to the percentage mucoadhesion, drug content, invitro drug release and permeation studies. F4 formulation was optimized with mucoadhesive force, %permeation efficiency and In-vitro drug release. Drug balls were characterized by FTIR and DSC study. Stability study revealed that the formulation was found to be stable.