scholarly journals Formulation Development and Optimization of Phase-Transition W/O Microemulsion In Situ Gelling System for Ocular Delivery of Timolol Maleate in the Treatment of Glaucoma

2020 ◽  
Vol 11 (2) ◽  
pp. 9097-9112
Keyword(s):  
Phase Transition ◽  
Drug Release ◽  
Zeta Potential ◽  
Open Angle Glaucoma ◽  
Ethyl Oleate ◽  
Stability Study ◽  
Class I ◽  
Formulation Development ◽  
Timolol Maleate

The present investigation is aimed to prepare and evaluate the micro emulsion-based phase transition ocular system for delivery of Timolol maleate in the treatment of glaucoma. Timolol maleate is used in the first line of treatment in open-angle glaucoma, belonging to BCS class-I having good solubility and permeability. The rapid precorneal elimination of conventional formulation containing class I drugs exhibits poor therapeutic effect and bioavailability. So, microemulsion (ME) based phase transition systems were formulated and characterized. ME based phase transition system was formulated using Ethyl oleate as oil and CremophorEL as a surfactant, Span 20 as Co-surfactant, and Sorbic acid as a preservative. These systems undergo a phase transition from water-in-oil (w/o) ME to liquid crystalline (LC) state and to coarse emulsion (EM) with a change in viscosity depending on dilution with tear fluid & water content. Prepared microemulsions were characterized for average globule size, zeta potential, pH, conductance, in-vitro gelling capacity. The optimized formulation was selected based on desirable attributes and was further characterized and compared with marketed ophthalmic gel-forming marketed solution of Timolol maleate (TIMOPTIC-XE®). All the results of the characterization were satisfactory. The optimized water-in-oil (w/o) microemulsion showed droplet size 23.47 nm, the zeta potential of 0.253mV, pH of 7.2, the conductance of 0.25mS, and drug content of 99.64%. The phase transition w/o ME provides the fluidity for installation with its viscosity being increased due to phase transition after application increasing ocular retention while retaining the therapeutic efficiency. The in- vitro drug release and IOP reduction with optimized formulation were found comparable and less fluctuating compared to marketed formulation. Optimized formulation was found stable during the accelerated stability study. The developed phase transition w/o ME formulation would be able to offer benefits, such as increased residence time, prolonged drug release, reduction in dosing frequency, and thereby it will improve patient compliance.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

scholarly journals Formulation, Optimization, and Characterization of Repaglinide Loaded Nanocrystal for Diabetes Therapy

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Gajanan Shinde ◽  
Mitesh Patel ◽  
Manan Mehta ◽  
Rajesh Kesarla ◽  
Ganesh Bangale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymer Concentration ◽  
Study Data ◽  
Stability Study ◽  
Diabetes Therapy ◽  
Peg 4000 ◽  
Number Of Cycles

The aim of the present investigation was to formulate and characterize nanocrystal formulation of Repaglinide for diabetes therapy. Formulation was done by high pressure homogenization. HPH pressure and cycles range were screened by preliminary batches (T1 and T2). 5, 8, and 10 cycles and 500 to 1500 bar pressure range had kept for further investigation. Taguchi design was used to optimize type of polymer, % polymer concentration, number of cycles, and HPH pressure for nanocrystal formulation. Formulations were characterized for particle size, zeta potential, and in vitro drug release. Optimized formulation (NC 3) showed particle size of 187 nm, zeta potential of −29.4 mv, and % drug release of 80.58% and it was used for further study. Data analysis proved significant effects of factors on responses. Polydispersity index (PDI) Analysis of optimized formulation were found to be 0.248. SEM showed nanocrystal aggregation of drug, may be due to water removal process. DSC showed slight change in crystallinity, may be due to the presence of PEG 4000. Stability study was carried out for 3 months. It indicated no significant change in particle size and zeta potential. However, further studies in higher animals and human being need to be performed before this formulation can be commercially exploited.

scholarly journals DESIGN EXPERT SUPPORTED FORMULATION DEVELOPMENT, MATHEMATICAL OPTIMIZATION AND PREDICTABILITY STUDY OF FLOATING TABLETS OF BISOPROLOL FUMARATE

2021 ◽  
pp. 242-248
Author(s):  
SHAIKH SHAOOR AHMAD ◽  
SHAIKH SIRAJ N. ◽  
PATEL M. SIDDIK ◽  
KHALIFA MAHMADASIF YUNUS ◽  
MAKRANI SHAHARUKH I. ◽  
...  
Keyword(s):  
Drug Release ◽  
Scale Up ◽  
Mathematical Optimization ◽  
Lag Time ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Floating Tablets ◽  
Design Expert

Objective: Focus of the study was to formulate Design expert Software assisted floating tablet of Bisoprolol Fumarate. Bisoprolol Fumarate is a Beta adrenergic blocking agent, used to treat cardiac diseases favorable characters to be formulated as sustained release Gastro retentive floating tablets. Methods: Floating Tablets of Bisoprolol Fumarate were prepared by using polymers such as Polyox N 12 K and Carbapol 940 P. Formulations were prepared by using direct compression method and evaluated for various parameters like Hradness, thickness, weight variations, Floating lag time Total floating time,% drug release and Stability Study etc. Results: FTIR spectroscopic study indicates no drug-excipients interaction in the prepared formulations. Hardness or crushing strength of the tablets of all the formulation was found between 5.8 and 6.5 kg/cm2. Floating lag time of all batches is in range of 1.18±2.0 to 2.43±1.6 (minutes). All other parameters of all batches are within an acceptable range. The polymer Carbopol 940 P had the significant negative effect of on the floating lag times. The In vitro dissolution profiles of optimized A3 Floating formulation of Bisoprolol Fumarate were found to sustain drug release 99.25 % up to 12 h with floating lag time of 1.45 min; Designed formulation was stable after Stability study. Optimization study was carried out by using 32 factorial designs to fabricate formulations. Conclusion: It can be conclude that reproducible results of various parameters in this developed formulation can easily scale up. Furthermore designed formulation will be very effective for controlling blood pressure.

scholarly journals “FORMULATION DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING FILMS OF LAFUTIDINE”

2019 ◽  
Vol 7 (2) ◽  
Author(s):  
Hir. R. Mehta ◽  
Vijay K. Patel
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Stability Study ◽  
Formulation Development ◽  
Casting Technique ◽  
Drug Content ◽  
Peg 400 ◽  
Weight Variation ◽  
Folding Endurance

The present invention was aimed to formulate and evaluate Lafutidine gastro retentive films. The films were prepared by solvent casting technique using different film forming polymers like HPMC and Ethyl cellulose. PEG 400 used as a plastsizer. The prepared films were evaluated for number of parameters like Physical appearance, Weight variation, Thickness, Folding endurance, Tensile strength, unfolding behavior, floating properties, drug content and In vitro drug release studies. From the trial batches the best release for gastroretentive film was shown by formulation T5 (Ethyl cellulose and PEG 400). Formulation T5 exhibited good appearance, better mechanical strength with acceptable flexibility. Also, formulation T5 was given more than 90 % drug released after 12 hr and 97.56 % Drug content.  For optimization of formulation, 32 factorial design was applied by taking Ethyl cellulose and PEG 400 as an independent variables. Drug release at 8 hour and folding endurance selected as dependent variables. Based on drug release study, L8 batch found most satisfactory in all formulation and the effect of Ethyl cellulose and PEG 400 found significant. L8 batch found stable during stability study. Key words: Lafutidine, Floating Films, Ethyl Cellulose.

scholarly journals Floating Microspheres Based Nizatidine Gastro Retentive Formulation to Control the Release of Drug

2020 ◽  
Vol 9 (3) ◽  
pp. 1409-1419
Keyword(s):  
Antimicrobial Activity ◽  
Drug Release ◽  
Zeta Potential ◽  
Surface Morphology ◽  
Zero Order ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Percentage Yield ◽  
Gastro Retentive

Present research aimed at formulation development and characterization of the floating drug delivery system of Nizatidine, a H2-receptor antagonist, widely prescribed in gastric ulcers and duodenal ulcers. Nizatidine loaded floating microspheres were developed by the solvent diffusion-evaporation method using polymers hydroxypropyl methylcellulose (HPMC) and microcrystalline cellulose (MCC) to prolong the gastric retention time of the drug for the therapeutic management of gastric disorders like ulcers. Further, the developed formulations were characterized for percentage yield, drug entrapment, floating behavior, shape and surface morphology, in vitro drug release, determination of particle size and Zeta potential, in vitro stability studies, and antimicrobial activity. The percentage yield of the different formulation was found to be a range of 75.65– 81.25%, drug entrapment efficacies of different formulations were in the range of 65.56- 75.65% w/w, formulation F4 of floating microsphere was found to be 178.5 nm, Zeta potential of optimized formulation F4 of floating microsphere was found -33.6 Mv, Surface morphology of formulation examines at two different magnification 55X which illustrate the smooth surface of Microspheres. The in vitro drug release pattern of Nizatidine loaded optimized floating microsphere was subjected to the goodness of fit test by linear regression analysis, and it was observed that ‘r’ values of microsphere were maximum for zero-order, i.e., 0.969 hence indicating drug release from formulations follow zero-order kinetics with non-fickian diffusion mechanism which in turn prolonged drug release. The antimicrobial activity of the optimized formulation showed clear fluid with no development of turbidity. It inferred better clearance from infection than plain drug solution at the same doses. Floating microspheres of Nizatidine as gastro retentive dosage forms precisely control the release rate of Nizatidine to a peculiar site and expedite an immense impact on health care.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF ELEMENTARY OSMOTIC TABLET OF LISINOPRIL DIHYDRATE

2017 ◽  
pp. 20-27
Author(s):  
BHUSHAN A. BHAIRAV ◽  
PRADNYA M. KHANDAGALE ◽  
R. B. SAUDAGAR
Keyword(s):  
Sodium Chloride ◽  
Drug Release ◽  
Release Rate ◽  
Flow Property ◽  
Stability Study ◽  
Formulation Development ◽  
Drug Release Rate ◽  
Accelerated Stability ◽  
Response Percentage

Objective: Lisinopril Dihydrate is one of the antihypertensive drug used to control the high blood pressure. Osmotically Controlled release tablet of Lisinopril Dihydrate was performed for reducing dosing frequency and patient compliance.Methods: Elementary osmotic tablets of Lisinopril Dihydrate were developed using Sodium chloride as a key ingredient which gives osmogent property which provides driving force inside the core tablet and which leads to release of the drug. Microcrystalline cellulose used as a release retardant material in the present work. Different formulations were prepared by varying the concentrations using 32 factorial designs. It was applied to see the effect of variables Sodium chloride (X1) and MCC (X2) on the response percentage drug release as a dependent variable. These formulations were evaluated for, Hardness, Flow property, Thickness, Friability, Drug content and In vitro drug release. Tablets were coated with a semipermeable membrane using 5% w/v cellulose acetate(CA) in acetone and PEG 400(1%) used as Plasticizer. Coated Elementary osmotic tablets were drilled for delivery orifice using a standard micro drill of diameter size 0.8 mm.Results: Drug release rate was increased as the increase in the concentration of sodium chloride and release rate decreased on increasing the concentration of MCC. Drug release rate was directly proportional to delivery orifice size. SEM Study carried out for detection of diameter size of the delivery orifice. The FTIR studies demonstrate that there was no interaction between polymer and drug.Conclusion: The optimized formulation was stable for 3 mo of accelerated stability study

scholarly journals FORMULATION, DEVELOPMENT, AND CHARACTERISATION OF CILNIDIPINE LOADED SOLID LIPID NANOPARTICLES

2018 ◽  
Vol 11 (9) ◽  
pp. 120
Author(s):  
Remya Pn ◽  
Damodharan N
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Tween 80 ◽  
Lipid Nanoparticles ◽  
Lipid Matrix ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Solid Lipid

Objective: The aim of the present investigation is to develop solid lipid nanoparticles (SLNs) of cilnidipine using hot homogenization followed by ultrasonication technique and to improve the dissolution characteristics of the drug.Methods: The cilnidipine-loaded SLNs were formulated using stearic acid (SA), glyceryl monostearate (GMS), and palmitic acid (PA) as lipid matrix and tween-20, tween-80, and tween-40 as an emulsifier by hot homogenization and ultrasonication method. The physicochemical characteristics of SLN were analyzed for Fourier transform infrared studies, entrapment efficiency (EE), zeta potential, in vitro drug release, particle size analysis, scanning electron microscopy, and stability.Results: The SLNs with PA showed a sustained release of drug 82%–88%, respectively, after 10 h. The SLNs of PA using tween-80 as emulsifier resulted with high EE% than SLNs of SA and GMS. The compatibility studies are done by Fourier transformed infrared for formulations which contain PA as lipid matrix and tween-80 as an emulsifier, and it showed no drug excipient incompatibility. The formulation containing PA and tween-80 shown particles of average size 152 nm having polydispersity index of. 217 with 68.7 % EE were produced. The zeta potential of the formulation was found to be – 27 mV and the order of percentage drug release was from PA>GMS>SA, and steric stabilizers retard the drug release more than ionic stabilizers.Conclusion: SLN formulations showed the best results in EE as well as in in vitro drug release and therefore confirmed that the novel drug delivery system provides an improved strategy for the treatment of hypertension.

scholarly journals Frovatriptan Succinate Loaded Lipid Nanoparticles: Formulation, Evaluation, Stability Study and Shelf Life Determination

2021 ◽  
pp. 266-274
Author(s):  
Mohd Yasir ◽  
Iti Chauhan ◽  
Madhu Verma ◽  
KM Noorulla ◽  
Abdurazak J. Tura ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Shelf Life ◽  
Lipid Nanoparticles ◽  
Stability Study ◽  
Burst Release ◽  
In Vitro Drug Release ◽  
Release Pattern

Aims: The aim of the research work was to prepare and optimize the Frovatriptan Succinate (FVN) loaded solid lipid nanoparticles. Methods: SLNs were developed by solvent  emulsification diffusion technique and evaluated for particle size, PDI, zeta potential, in-vitro drug release, and finally stability study was conducted for the detection of shelf life. Results: The optimized formulation exhibited particle size, PDI, and zeta potential 122.85±9.24 nm, 0.129 and -25.85 mV, respectively.  In-vitro drug release study exhibited  biphasic drug release pattern.  Initially (in first two hrs) the drug was release in fast manor i.e. burst release (32.36±7.28 %). It might be due to the presence of drug on the surface of SLNs. After  2 hrs of study, the release pattern became sustained up to 24 hrs. The total amount of drug release in 24 h was found to be 91.29 ± 8.26%.  Various kinetic models were applied to evaluate the release pattern of the drug form the formulation.  Higuchi model was found to be the best fitted with the R2 value of 0.9482. The release mechanism was found to be the Fickian type with the release exponent (n) value of 0.4386. Finally, stability study was conducted. The formulation was found to be the stable under the studied conditions. The shelf life of the formulation was found to be 1.77 years. Conclusion: Finally, it could be concluded that, the SLNs are the suitable carrier for the delivery of FVN .

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF pH TRIGGERED IN SITU OPHTHALMIC GEL OF BESIFLOXACIN HYDROCHLORIDE

2018 ◽  
Vol 8 (5) ◽  
pp. 313-321 ◽  
Author(s):  
Vishakha Waghulde ◽  
Ravindranath Saudagar
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Drug Release ◽  
Stability Study ◽  
Gelling Agent ◽  
Formulation Development ◽  
Drug Content ◽  
Wide Range

The aim of the present work was to formulation and evaluation of pH Triggered in-situ Ophthalmic Gel of Besifloxacin Hydrochloride to overcome the drawbacks obtained by conventional eye drop. There are two independent variables were used i.e. Carbopol 934 and HPMC K100. Carbopol 934 were used as gelling agent and HPMC K100 were used as bioadhesive polymer. Besifloxacin Hydrochloride shows activity against a wide range of Gram-positive and negative ocular pathogens: examples are  Corynebacterium pseudodiphtheriticum, Moraxella lacunata, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae and Streptococcus salivarius. The in situ gelling system involves sol-to-gel transition in the cul-de-sac upon instillation to avoid pre corneal elimination. The formulations were prepared by 32 factorial design. The prepared formulations were evaluated for clarity, pH, viscosity, Bioadhesive strength of gel, gel strength gel, Drug Content, In-vitro Drug Release Study, Antibacterial Activity, Isotonicity Evaluation, HET-CAM Test and stability studies. The drug content was in the range of 97-99.57 %. Formulation F5 selected as optimized on the basis of evaluation. It shows highest drug release upto 8hrs. It shows good antibiotic activity against Staphylococcus aureus. The optimized formulation was isotonic with blood cells. It passes sterility test. The optimized formulation passes the ocular irritancy test i.e. HET-CAM Test. The formulation kept for the stability study for 3 months. Short term stability study indicates that room temperature 400±20 was appropriate storage condition for formulations. Keywords: pH Triggered, bioadhesive polymer, Carbopol 934, HPMC K100, HET-CAM Test, Antibacterial Activity.

scholarly journals FORMULATION AND EVALUATION OF NANOSTRUCTURED LIPID CARRIERS BASED ANTI-INFLAMMATORY GEL FOR TOPICAL DRUG DELIVERY SYSTEM

2019 ◽  
pp. 286-291
Author(s):  
ROHINI S KHARWADE ◽  
NILESH M MAHAJAN
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Stability Study ◽  
Nanostructured Lipid Carrier ◽  
Topical Gel ◽  
Rat Paw Edema

Objective: Nanostructured lipid carrier (NLC)-based topical gel of lornoxicam (LXM) was formulated with the aim of controlled release action and to reduce systemic side effect for the treatment of an arthritic condition. Methods: NLCs developed using high-pressure homogenization method and optimized using a 32 factorial design with response surface methodology using design expert software. NLCs were characterized for particle size, zeta potential analysis, drug entrapment efficiency, and in vitro drug release studies to select the optimized formulation. The NLCs were suitably gelled and evaluated with respect to homogeneity, pH, viscosity, gel strength, spreadability, rheological characteristics, drug content, in vitro diffusion, and stability study. Safety of the NLC-based gel was assessed using primary skin irritation studies, and efficacy was confirmed using carrageenan-induced rat paw edema model. Results: NLCs formulation comprising 2% of lipid (60:40) and surfactant (1.50%) was confirmed as an optimized batch having a particle size (138.2±3.60 nm) with polydispersibility index value 0.344±0.034. The zeta potential value indicates good physical stability. Based on the results from the in vitro release study it was shown that the formed gels had the ability to extend release of LXM for 24 h and showing percentage drug release of 90.92%±1.96% at the end of 24 h. Skin irritation studies revealed that the optimized gel formulation shows no erythema, edema, or ulceration. Conclusion: The overall results of the present study clearly indicated promising potentials of NLC-based gel for delivering LXM topically over the conventional gel.

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