scholarly journals FORMULATION AND EVALUATION OF TOPICAL NANOEMULGEL OF METHOTREXATE FOR RHEUMATOID ARTHRITIS

2021 ◽  
pp. 351-357
Author(s):  
SAHELI DAS ◽  
SHARADHA M. ◽  
M. P. VENKATESH ◽  
SUBHASHREE SAHOO ◽  
JOGABRATA TRIPATHY ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Particle Size ◽  
Ternary Phase Diagram ◽  
Release Kinetics ◽  
Stability Study ◽  
Peanut Oil ◽  
Tween 20 ◽  
Spontaneous Emulsification ◽  
Drug Content ◽  
Peg 400

Objective: The purpose of this study was to develop and evaluate methotrexate-loaded nanoemulgel for topical delivery in the management of rheumatoid arthritis. Methods: Based on nanoemulsion composition, the pseudo ternary phase diagram was fabricated by using peanut oil, Tween 20 as the surfactant, and PEG 400 being used as a co-surfactant. The methotrexate-loaded nanoemulsion was formulated by using the spontaneous emulsification method. Badam gum was used as a gel matrix in the prepared nanoemulsion to form nanoemulgel. The methotrexate loaded nanoemulgel was characterized and evaluated for pH, particle size, physical appearance, viscosity, spreadability, TEM, drug content, diffusion study, release kinetics, and stability studies. Results: The nanoemulgel constituting 8.6% peanut oil, 34.4% of Tween 20 and PEG 400 as Smix (surfactant and co-surfactant mixture), 43% water, and 12.5% w/w badam gum was concluded as optimized formulation. The prepared nanoemulgel was translucent in nature having a particle size of 195.1nm and zeta potential of -0.278mV. Drug content and drug release for the optimized formulation were found to be 98.11±0.34% and 95.11±0.02% respectively. pH, viscosity, and spreadability were found to be optimum. Stability study data showed that the prepared nanoemulgel was stable at different temperatures varying from -25 to +45ºC. Conclusion: Methotrexate loaded nanoemulgel has been formulated for topical drug delivery for the management of rheumatoid arthritis.

scholarly journals EVALUATION OF STABILITY OF ROPINIROLE HYDROCHLORIDE AND PRAMIPEXOLE DIHYDROCHLORIDE MICROSPHERES AT ACCELERATED CONDITION

2018 ◽  
Vol 10 (4) ◽  
pp. 82
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
Gouranga Nandi
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Shelf Life ◽  
Stability Study ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Ropinirole Hydrochloride ◽  
Pramipexole Dihydrochloride

Objective: The objective of the present work was to conduct accelerated stability study as per international council for harmonisation (ICH) guidelines and to establish shelf life of controlled release dosage form of ropinirole hydrochloride and pramipexole dihydrochloride microspheres for a period of 6 mo.Methods: Most optimized batch of ropinirole hydrochloride and pramipexole dihydrochloride (F12 and M12 respectively) were selected and subjected to exhaustive stability testing by keeping the sample in stability oven for a period of 3 and 6 mo. Various parameters like surface morphology, particle size, drug content, in vitro drug release and shelf life were evaluated at 3 and 6 mo period. The surface morphology of the formulated microspheres was determined by scanning electron microscopy (SEM). The particle size of the microspheres was estimated by optical microscopy method. The drug content was assayed by the help of ultra-violet spectrophotometer (UV). The in vitro drug release was performed by using Paddle II type dissolution apparatus and the filtrate was analyzed by UV spectrophotometer. The shelf life of the optimized microspheres was calculated by using the rate constant value of the zero-order reaction.Results: A minor change was recorded in average particle size of F12 and M12 microspheres after storage for 6 mo. For F12 and M12, initially the particle size was 130.00 µm and 128.92 µm respectively and after 6 mo it was found to be 130.92 µm and 128.99 µm respectively. There was no change in surface morphology of F12 and M12 microspheres after 6 mo of storage. The shape of microspheres remained spherical and smooth after 6 mo. An insignificant difference of drug content was recorded after 6 mo compared to the freshly prepared formulation. For F12 and M12, 94.50% and 93.77% of the drug was present initially and after 6 mo 94.45% and 93.72% of the drug was recorded. In vitro drug release was recorded after 6 mo for F12 and M12. Initially, 97.99% and 97.69% of the drug was released till 14th hour respectively for F12 and M12. After 6 mo, 98.23% and 97.99% of the drug was released respectively. The percentage residual drug content revealed that the degradation of microspheres was low. Considering the initial percentage residual drug content as 100%, 99.94% of the drug was recorded for both F12 and M12. The shelf life for F12 and M12 was found to be 10 y 52 d and 10 y 70 d respectively which were determined by the zero-order kinetic equation.Conclusion: A more or less similar surface morphology, particle size, drug content and percent of drug release before and after stability study confirmed the stability of F12 and M12 microspheres after storage for 6 mo and prove the efficacy of the microspheres in the site-specific delivery of drugs in Parkinson’s disease.

FORMULATION AND EVALUATION OF NATEGLINIDE NANOSPONGES

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (02) ◽  
pp. 27-35
Author(s):  
A. A Bakliwal ◽  
◽  
D. S. Jat ◽  
S. G. Talele ◽  
A. G. Jadhav
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Synthesis Method ◽  
Ultra Sound ◽  
Size Analysis ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Drug Content

The objective of the present study was to produce extended release nateglinide nanosponges for oral delivery. Preparation of nanosponges leads to solubility enhancement. Nateglinide is a BCS Class II drug, having low solubility. So, to increase the solubility of nateglinide it is formulated into nanosponges. Nanosponges using ethyl cellulose as a polymer and dichloromethane as a cross-linker were prepared successfully by ultra-sound assisted synthesis method. The effects of different drug: placebo ratios on the physical characteristics of the nanosponges as well as the drug content and in vitro drug release of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning and transmission electron microscopy of nanosponges showed that they were spongy in nature. The particle size was found to be in the range 46.37 - 97.23 nm out of which particle size of the optimized formulation was 51.79 nm and the drug content was found to 79.43 %. The optimized nanosponge formulations were selected for preparing nanosponge tablets for extended drug delivery by oral route. These tablets were prepared using xanthan gum and PVP K-30 and were evaluated by pre-compression and post-compression parameters. The nateglinide nanosponges tablet formulation were studied for different parameters using Design Expert Software. All formulations were evaluated for in vitro drug release analyzed according to various release kinetic models and it was found that it follows zero order release kinetics.

scholarly journals Development and Characterization of Ofloxacin & Prednisolone Loaded Nanostructured Lipid Carriers (Nlc) for Topical Route

2019 ◽  
Vol 4 (1) ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Morphological Characteristics ◽  
Nanostructured Lipid Carriers ◽  
Diffusion Method ◽  
Prolonged Release ◽  
In Vitro Drug Release ◽  
Drug Content

Aim: The present study was designed to develop and characterize nanostructured lipid carriers (NLC) of Ofloxacin and Prednisolone for topical use in case of infections associated with inflammation. Materials and Methods: Ofloxacin was obtained as gift sample from Mankind Pharma Ltd, VillKyarta, P.O. Misserwal, Poonta Sahib, Sir Mour. H.P. Whereas Prednisolone was purchased from Yarrow chem., Mumbai. It was evaluated for its pre-formulation studies (organoleptic properties, melting point, solubility, compatibility, max. wavelength of absorption). NLCs were prepared through melt-emulsification followed by ultra-sonication technique. Further optimized batch of NLCs was incorporated into Gel. Formulated NLCs were evaluated in terms of morphological characteristics, particle size (Polydispersity Index), drug content, In-vitro drug release (using egg membrane), drug release kinetics (Ritger-Peppas diffusion method). Finally, gel containing NLCs was studied by physical characteristics, pH, viscosity, spreadability, drug content, In-vitro drug release and its kinetics. Results and Discussion: In pre-formulation study, drugs were found having the similar properties as described in Indian Pharmacopoeia (IP) and United States Pharmacopoeia (USP). SEM photomicrograph revealed that NLCs were spherical with more or less smooth surface; particle size 512.3-1703 nm and PDI- 0.399-0.742 (ofloxacin) and particle size 539.3-1736.7 nm and PDI- 0.335 - 0.711 (prednisolone);drug content was found in range of 56.7 - 75.6% for ofloxacin and 65.9 – 81.8% for prednisolone. NLC1 demonstrated maximum release rate with 83.37±1.70% and NLC8 73.96±0.53%.NLC6 was best fitted in Korsmeyer - peppas model as the regression coefficients were 0.960, 0.964, 0.977, 0.950, 0.980 & 0.987 respectively and prednisolone NLC 9 (0.953) and they were close to 1. Conclusion: In conclusion, the prepared NLCs had prolonged release effects with good potential for topical delivery of NLC based gel formulation of ofloxacin& prednisolone.

scholarly journals Oral Formulation of Anticancer Agents for Colon Cancer

2021 ◽  
pp. 402-418
Author(s):  
Dipti Patel ◽  
Krishna Patel
Keyword(s):  
Colon Cancer ◽  
Particle Size ◽  
Anticancer Agents ◽  
Crosslinking Agent ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Inlet Temperature ◽  
Disintegration Time ◽  
Drug Content ◽  
Enteric Coated

Aims/Objective: To develop and estimate enteric-coated capsules containing mucoadhesive Microspheres of Capecitabine and Oxaliplatin to treat Colon cancer. Study Design: Box Behnken. Place and Duration of Study: Department of Pharmaceutics, Parul Institute of Pharmacy and Research, Parul University, Vadodara, between 2017 to 2021. Methodology: Capecitabine and Oxaliplatin are used as antineoplastic agents and can be delivered via the oral route of administration. For the estimation of drugs Analytical method has been developed by HPLC. Box Behnken design has been used to optimize Drug: polymer ratio (1:2), Inlet temperature 170ºC, and crosslinking agent with a 0.5 ml 1% Gluteraldehyde solution. The microspheres were successfully prepared by using the spray drying technique and evaluated. Results: The results of optimized Capecitabine microspheres were obtained as Particle size 87.91 µm ± 0.274,% yield 57.21± 1.5,% Mucoadhesion 57.21± 1.5,% entrapment efficiency 82.16± 0.725. The results of optimized Oxaliplatin microspheres were obtained as Particle size 99.88µm±0.034,% yield 56.0± 0.088,% Mucoadhesion 87.0± 0.80,% entrapment efficiency 82.61±0.085. The drug content of Capecitabine and Oxaliplatin in the filled capsule was 94.67% ±0.32 and 93.45%±0.712, respectively. % Drug release of Capecitabine and Oxaliplatin in Phosphate buffer pH 7.4 was found to be 94.83±0.22 and 96.94±0.11 respectively after 8 hrs. Stability study at 400C±20C / 75 ± 5 % RH revealed that there was no significant change in disintegration time, drug content and % CDR during 6 months. So, prepared formulation was stable during stability study.  MTT assay has been performed on the formulation of Capecitabine and Oxaliplatin microspheres for assessing the % viability of both the drugs on the Caco-2 cell line. Conclusion: The present study confirmed that prepared mucoadhesive microspheres filled with enteric-coated capsules have an antitumor effect on colon cancer cells. The formulation induced high cell death within 48 hours, and less cell viability was obtained compared to API. Six months accelerated Stability study indicates that formulation is fairly stable at storage conditions.

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 Formulation and in vitro Assessment of Eudragit L 100 and Eudragit S 100 Based Naproxen Microspheres

2016 ◽  
Vol 15 (1) ◽  
pp. 47-55
Author(s):  
Md Ataur Rahman ◽  
Nusrat Ahmed ◽  
Ikramul Hasan ◽  
Md Selim Reza
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Product Yield ◽  
Drug Content ◽  
S 100 ◽  
Emulsification Solvent Evaporation ◽  
Eudragit S 100

In the present study naproxen loaded microspheres were prepared by emulsification solvent evaporation method in order to achieve targeted drug delivery. Eudragit L 100 and Eudragit S 100 were used as the rate retardant polymers in the preparations. Thirteen formulations (F1-F13) were prepared using 22 factorial design by changing the concentration of these two polymers. All the formulations were evaluated for product yield, drug content, entrapment efficiency, particle size and drug release profiles. Highest drug content and entrapment efficiency were found to be 30.17% (F4) and 91.86% (F8) respectively. The particle size was found to be 159.26-234.70 ?m for all formulations. In-vitro drug release studies were performed using USP type II (Paddle) apparatus for 8 hrs in pH 7.4 phosphate buffer. The maximum drug release after 8 hrs was found to be 60.19% for batch F4. The release kinetics of all formulations were evaluated by using zero order, first order, Higuchi, Korsmeyer-Peppas, Kopcha and Hixson Crowell model. Almost all formulations fitted best with the Kopcha kinetic model. The SEM study indicated the spherical structure of the microspheres having rough surfaces.Dhaka Univ. J. Pharm. Sci. 15(1): 47-55, 2016 (June)

scholarly journals OPTIMASI PEMBUATAN NANOEMULSI VIRGIN COCONUT OIL

Jurnal Kimia ◽  
2018 ◽  
pp. 8
Author(s):  
N. M. D. Listyorini ◽  
N. L. P. D. Wijayanti ◽  
K. Widnyani Astuti
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Coconut Oil ◽  
Tween 20 ◽  
Virgin Coconut Oil ◽  
Spontaneous Emulsification ◽  
Peg 400

Penelitian ini mempelajari optimasi pembuatan nanoemulsi menggunakan virgin coconut oil (VCO) yang bertujuan untuk memperoleh perbandingan minyak (VCO), surfaktan dan kosurfaktan yang dapat membentuk nanoemulsi yang memenuhi persyaratan menggunakan Self Nano-Emulsifying Drug Delivery System (SNEDDS). Metode yang digunakan adalah Spontaneous Emulsification yang termasuk ke dalam SNEDDS. Perbandingan yang digunakan dalam nanoemulsi yaitu minyak (VCO): surfaktan (Cremophor RH40 atau Tween 20): kosurfaktan (PEG 400 atau etanol): fase air (akua deion) dengan perbandingan (1:8:1):5, (1:7:2):5 dan (2:7:1):5 yang menghasilkan 12 buah formula. Dilakukan uji evaluasi berupa uji stabilitas isik dan persen transmitan ke-12 formula. Diperoleh 2 formula yang dilanjutkan untuk uji zeta potensial dan ukuran partikel yaitu F2 dan F7. Uji zeta potensial F2 (0,14 mV) dan F7 (0,48 mV) serta uji ukuran partikel F2 (20,8 nm) dan F7 (20,6 nm). Berdasarkan hasil uji evaluasi yang dilakukan maka diperoleh dua formula yaitu F2 (VCO: Cremophor RH40: PEG 400 (1: 8:1)) dan F7 (VCO: Cremophor RH40: Etanol (1: 7: 2)) yang sesuai persyaratan untuk menghasilkan nanoemulsi yang baik.

scholarly journals FORMULATION AND EVALUATION OF NANOEMULSION FOR TOPICAL APPLICATION

2019 ◽  
Vol 9 (4-s) ◽  
pp. 370-375
Author(s):  
Neha M Shaikh ◽  
S. M. Vijayendra Swamy ◽  
NAGOBA SHIVAPPA NARSING ◽  
K B Kulkarni
Keyword(s):  
Drug Efficacy ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Tween 20 ◽  
Topical Formulation ◽  
Spontaneous Emulsification ◽  
Poor Solubility ◽  
Tinea Versicolor ◽  
Econazole Nitrate

The aim of present research is to design and develop nanoemulsion of Econazole nitrate as effective treatment for tinea versicolor fungal disease. Econazole nitrate is an imidazole antifungal agent with broad spectrum activity. It belongs to BCS class II i.e. low soluble and highly permeable drug. Due to its poor solubility, it is incompletely absorbed after oral dosing and bioavailability varies among individuals. The drug efficacy of topical formulation can be limited by instability due to its poor solubility in the vehicle and low permeability. Therefore, to overcome these problems nanoemulsions have been designed. Topical nanoemulsion containing 1 % Econazole nitrate with different oils (oleic acid), surfactant (tween 20), co-surfactant (PEG 200, PEG 400) and distilled water. Various oil-in-water nanoemulsions are prepared by the spontaneous emulsification method. The nanoemulsion formulations that passed thermodynamic stability tests were characterized for appearance, pH, FTIR, viscosity, drug content, % drug entrapment efficiency and in-vitro drug release study of Econazole nitrate determined by Franz diffusion cell and stability study.

scholarly journals Formulation and in-vitro evaluation of Glipizide (Anti diabetic drug) Liposphere

2018 ◽  
Vol 8 (6-s) ◽  
pp. 116-119
Author(s):  
Sarika Saini ◽  
Aman Mittal
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Paraffin Wax ◽  
Drug Content ◽  
Dissolution Apparatus ◽  
Dispersion Technique

Objective- The aim of the present study was to formulate and in- vitro study of glipizide liposphere by using melt dispersion technique. Methods- Glipizide Liposphere system composed of paraffin wax, Stearic acid as lipid phase and sodium lauryl sulphate as surfactant. Glipizide lipospheres were prepared by using melt dispersion technique. Formulation of Glipizide was evaluated such as organoleptic properties, particle size, drug content, entrapment efficiency in-vitro study and stability of the lipospheres. Result- The formation of glipizide lipospheres by using melt dispersion technique was done successfully. All the formulations have off- white in colour, characteristic odour and spherical shape. The formulation A4 has particle size 19.65 μm, drug content 84.93 %, entrapment efficiency 80.75 % and the percentage drug release was carried out by using USP type 2 dissolution apparatus in 6.8 pH phosphate buffer solution and drug release of glipizide lipospheres within 12 hrs was found to be 74.06 %.stability study of glipizide lipospheres revealed that the formulation was stable at 5oC ± 3oC. Keywords- Lipospheres, Glipizide, Paraffin wax, Melt dispersion method, Dissolution Apparatus, Stability study

scholarly journals Development and evaluation of medicated cosmetic cream to produce triple effect on skin for the treatment of uneven skin tone

2020 ◽  
Vol 11 (1) ◽  
pp. 221-232
Author(s):  
Sharadha M ◽  
D V Gowda ◽  
Famna Roohi N K
Keyword(s):  
Particle Size ◽  
Chemical Interaction ◽  
Release Kinetics ◽  
Size Analysis ◽  
Dermal Toxicity ◽  
Scanning Calorimetry ◽  
Drug Content ◽  
Toxicity Studies ◽  
Percentage Yield ◽  
Ft Ir

Combinations of drugs are available in the market only to produce a single effect. To overcome this, a combination of three drugs namely α-arbutin, glutathione, and grape seed extract, are used to benefit the triple effect on the skin. The set forth study to formulate and evaluate medicated cosmetic cream in an effective curative strategy for derma to produce a triple effect. Medicated cosmetic cream containing triple bioactive agents formulated by the O/W dispersion method. Fourier transform infrared (FT-IR) and differential scanning calorimetry (DSC) was carried out for characterization. The formulated cream assessed for physical appearance, homogeneity, pH, viscosity, particle size analysis, spreadability, percentage yield, drug content, diffusion studies, release kinetics, acute dermal toxicity studies, and short-term stability studies. FT-IR and DSC studies revealed that no chemical interaction existed between the drug and excipients used. The optimized formula A5 revealed to be off white, semisolid, pleasant odor, smooth & slippery texture, non-greasy smear, easy to remove, and homogenous. The A5 cream exhibited a pH of 5.89, Viscosity of 1597.73 CPS, Spreadability of 20.86 g.cm/sec., the Particle size of 0.237%, Percentage yield of 98.8%, Drug content of 99.22 at 289 nm, 99.75 at 200 nm and 100.1 at 286 nm. The optimized cream demonstrated prolonged drug release 94.41% at 289 nm, 92.68 at 200 nm, and 92.78 at 286 nm up to 12 hrs. The optimized cream remained stable after the heating-cooling cycle at 4° C, 45° C and at room temperature. Furthermore, acute dermal toxicity studies showed the optimized formulation to be non-irritant, with no erythema, and no edema. The present study signified that the multiple combinations showed a better synergistic effect, superior efficacy, and multiple activities that resulted in the best, smooth, and stable medicated cosmetic cream.

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