scholarly journals Comparative study for optimization of folic acid nanoparticles

2020 ◽  
Vol 10 (2) ◽  
pp. 5156-5160
Keyword(s):  
Drug Release ◽  
Comparative Study ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Liquid Paraffin ◽  
Amorphous Structure ◽  
Long Term Stability ◽  
Refrigerator Temperature ◽  
The Stability

The present comparative study aims at studying the effect of several adjuvents on enhancing the stability and sustainability of FA NLCs which previously showed very promising results. The problem was encountered in the high drug release, high skin permeation, low deposition and low stability. In the present study, propylene glycol was added to all preparations as a stabilizer and coemulsifier. Plurol® stearique was utilized as solid lipid and stabilizer instead of apifil®. Soft paraffin was used as a softening additional lipid to Plurol® stearique to ensure the amorphous structure of NLCs. Liquid paraffin was used for its emollient effect instead of capryol ™ 90 with Apifil®. The in vitro drug release, ex vivo drug permeation and skin deposition were analyzed. Selection of the most optimum formulation is achieved to investigate its photostability, long term stability. Also, it was photographed under TEM. The selected formulation was stable after six hours of irradiation. The optimized selected formulation was successfully stable in refrigerator temperature throughout 9 months of the study. The TEM photograph reveals the formation of rounded nano vesicles. The present study was successful in development of more stable, more sustained means for topical delivery of FA for future cosmoceutical benefits.

scholarly journals DEVELOPMENT AND EVALUATION OF TRANSDERMAL FILM CONTAINING SOLID LIPID NANOPARTICLES OF RIVASTIGMINE TARTRATE

2017 ◽  
Vol 9 (6) ◽  
pp. 85
Author(s):  
G. Ravi ◽  
N. Vishal Gupta
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Cost Effective ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Study Results ◽  
Transdermal Film

Objective: The objective of present investigation was to develop rivastigmine tartrate transdermal film employing factorial design.Methods: The formulations were designed by Design-Expert software-version10. A series of films were prepared by solvent casting method using polymers, plasticizer, permeation enhancer and other solvents. Transdermal films were evaluated for flatness, drug content, tensile strength, in vitro drug release and ex vivo skin permeation study.Results: The flatness was found 100% (percentage) for all film formulations. The drug content of transdermal film was found in the range of 96.51±0.2 to 98.81±0.3%. The tensile strength of transdermal film was found in the range of 6.28±0.06 to 11.56±0.03 N/mm2 (newton/millimeter2) and in vitro drug release at 24th h (hour) was found in the range of 86.24±0.25 to 96.1±0.48%% for various formulations and ex vivo skin permeation study results at 24th h was found in the range of 85.83±0.74 to 97.36±0.93%.Conclusion: These results support the feasibility of developing transdermal film of rivastigmine tartrate for human applications. Thus, transdermal delivery of rivastigmine tartrate film is a safe, painless and cost effective drug delivery system for Alzheimer’s patients.

scholarly journals Development and Optimization of Proniosomal Gel Containing Etodolac: In-vitro, Ex-vivo and In-vivo Evaluation

2021 ◽  
Vol 62 (3) ◽  
pp. 290-304
Author(s):  
Moreshwar Patil ◽  
Prashant Pandit ◽  
Pavan Udavant ◽  
Sandeep Sonawane ◽  
Deepak Bhambere
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
In Vivo Evaluation ◽  
Vesicle Size ◽  
Skin Delivery ◽  
The Stability

Introduction: Etodolac is used in the treatment of acute pain and inflammation. It has low solubility because of high hydrophobicity and it is reported that upon oral administration shows gastric disturbances. This encourages the development of topical vesicular formulation. Method: In this work we used coacervation-phase separation method for the development of etodolac loaded vesicular system by using non-ionic surfactants, cholesterol and soya lecithin. Central composite design (rotatble) was used to optimize the concentrations of soy lecithin, surfactant and cholesterol. The prepared formulations were characterized by number of vesicles formed, vesicle size, zeta potential, entrapment efficiency, in-vitro permeation, ex-vivo permeation and anti-inflammatory study. Results: Etodolac was successfully entrapped in all formulations having efficiency in the range of 74.36% to 90.85%, which was more at 4 °C than room temperature. When hydrated with water; niosome in the range of 54 to 141 (per cubic mm) were spontaneously produced. The results of in-vitro diffusion study revealed that etodolac was released in the range of 71.86 to 97.16% over a period of 24 hrs. The average vesicle size of optimized formulation was found 211.9 nm with PDI of 0.5. The observed responses i.e. % encapsulation efficiency and drug release were 74.12 and 95.08 respectively. The zeta potential was -19.4mV revealed the stability of formulation which was further confirmed by no changes in drug content and drug release after stability studies. The % inhibition in paw volume was 40.52% and 43.61% for test and marketed proniosomal gel. Conclusion: Proniosomal gel formulation was stable and could enhance skin delivery of etodolac because of excellent permeation capability of vesicular system.

scholarly journals Development and Evaluations of Transdermally Delivered Luteolin Loaded Cationic Nanoemulsion: In Vitro and Ex Vivo Evaluations

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1218
Author(s):  
Mohammad A. Altamimi ◽  
Afzal Hussain ◽  
Sultan Alshehri ◽  
Syed Sarim Imam ◽  
Usamah Abdulrahman Alnemer
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Transdermal Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Oral Drug ◽  
In Vitro Drug Release ◽  
Drug Deposition ◽  
Drug Content

Introduction: Luteolin (LUT) is natural flavonoid with multiple therapeutic potentials and is explored for transdermal delivery using a nanocarrier system. LUT loaded cationic nanoemulsions (CNE1–CNE9) using bergamot oil (BO) were developed, optimized, and characterized in terms of in vitro and ex vivo parameters for improved permeation. Materials and methods: The solubility study of LUT was carried out in selected excipients, namely BO, cremophor EL (CEL as surfactant), labrasol (LAB), and oleylamine (OA as cationic charge inducer). Formulations were characterized with globular size, polydispersity index (PDI), zeta potential, pH, and thermodynamic stability studies. The optimized formulation (CNE4) was selected for comparative investigations (% transmittance as %T, morphology, chemical compatibility, drug content, in vitro % drug release, ex vivo skin permeation, and drug deposition, DD) against ANE4 (anionic nanoemulsion for comparison) and drug suspension (DS). Results: Formulations such as CNE1–CNE9 and ANE4 (except CNE6 and CNE8) were found to be stable. The optimized CNE4 based on the lowest value of globular size (112 nm), minimum PDI (0.15), and optimum zeta potential (+26 mV) was selected for comparative assessment against ANE4 and DS. The %T values of CNE1–CNE9 were found to be ˃95% and CEL content slightly improved the %T value. The spherical CNE4 was compatible with excipients and showed % total drug content in the range of 97.9–99.7%. In vitro drug release values from CNE4 and ANE4 were significantly higher than DS. Moreover, permeation flux (138.82 ± 8.4 µg/cm2·h), enhancement ratio (8.23), and DD (10.98%) were remarkably higher than DS. Thus, ex vivo parameters were relatively high as compared to DS which may be attributed to nanonization, surfactant-mediated reversible changes in skin lipid matrix, and electrostatic interaction of nanoglobules with the cellular surface. Conclusion: Transdermal delivery of LUT can be a suitable alternative to oral drug delivery for augmented skin permeation and drug deposition.

scholarly journals FORMULATION AND EVALUATION OF LORAZEPAM ENCAPSULATED COLLAGEN/PECTIN BUCCAL PATCH

2019 ◽  
pp. 200-209
Author(s):  
LAKSHMI V. S. ◽  
REVATHY B. MENON ◽  
KEERTHANA RAJU ◽  
AISWARYA M. U. ◽  
SREEJA C. NAIR
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Epileptic Seizures ◽  
Stability Study ◽  
Histopathological Study ◽  
In Vitro Drug Release ◽  
Control Drug ◽  
Ex Vivo Permeation Study ◽  
The Stability

Objective: To formulate and characterize Lorazepam loaded buccal patches using mucoadhesive, biodegradable, natural polymers-pectin (hydrophilic) and collagen (lipophilic) for treating epileptic seizures. Methods: Lorazepam loaded buccal patches were prepared by solvent casting method and were subjected to various Physico-chemical evaluation parameters to find the optimized buccal patch. The in vitro drug release study and ex vivo permeation study was carried out. The stability study and histopathological study of optimized Lorazepam loaded buccal patch was also carried out. Results: From in vitro drug release study, it was found that Lorazepam loaded buccal patch (B4) exhibited maximum drug release of 96.16 %±0.07 than other formulations at the end of 4 h, indicating an initial burst release followed by sustained release with release kinetics as Higuchi diffusion model. Based on the in vitro drug release, % drug content, % swelling index, folding endurance, B4 formulation was considered as optimised formulation and was further characterized. Ex vivo permeation study revealed that the cumulative amount of drug permeated from optimised Lorazepam loaded buccal patch (B4) was higher (3831.4±0.21µg/cm2) than marketed Midazolam buccal solution (1724±0.12 µg/cm2) and control drug solution (895.42±0.07 µg/cm2) with an enhancement ratio of 4.8. B4 formulation also showed a higher flux value (12.52±0.02µg/cm2/hr) compared to marketed formulation (5.732±0.01 µg/cm2) and control drug solution (2.563±0.03 µg/cm2) of P<0.05. The histopathological study using bovine buccal mucosa revealed that the B4 formulation is safe for buccal application. The stability study confirmed that B4 formulation is stable in both room and refrigeration conditions. Hence the formulated Lorazepam loaded buccal patch seems to be a promising carrier for the enhanced buccal delivery of Lorazepam in treating epileptic seizures. Conclusion: The formulated Lorazepam loaded collagen/pectin buccal patch was found to be an efficient and stable route for the buccal delivery of Lorazepam in treating acute epileptic seizures which could be further explored scientifically.

scholarly journals Formulation and Evaluation of Minoxidil Gel Using Acrylamide/Sodium Acryloyldimethyl taurate copolymer for Alopecia areata

2018 ◽  
Vol 10 (01) ◽  
Author(s):  
Shailendra Kumar Singh ◽  
Pawan Kumar ◽  
Deepak Kumar Jindal ◽  
Vandana Handa ◽  
Jyoti Bilonia
Keyword(s):  
Drug Release ◽  
Alopecia Areata ◽  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Chronic Inflammatory Disease ◽  
Effective Dosage ◽  
World Population ◽  
Drug Content

Alopecia areata is a common, chronic inflammatory disease, characterized by patchy hair loss on the scalp, affecting about 2.1% of world population. Presently, minoxidil has been used for treatment of alopecia as topical lotion, but associated with many drawbacks like systemic side effects and low contact time with skin. Therefore, in the present work, minoxidil gel was prepared using a novel copolymer, Sepineo P 600 to overcome these drawbacks. The prepared gel was characterized for pH, drug content, viscosity, spreadability, skin adhesivity, occlusivity, in vitro drug release, ex vivo skin permeation, stability and finally for skin corrosivity. The drug content of the finalized gel was found to be 99.80 ± 0.82%. The formulation showed good spreadability, occlusivity, adhesiveness and viscosity. In vitro release studies showed that the drug release from prepared gel followed matrix release pattern as compared to lotion. Mathematical modelling of the drug release data suggested Higuchi release model. The formulated minoxidil gel was found to be non-corrosive and stable when subjected to accelerate as well as real time stability studies. Overall, the minoxidil gel formulation was suitable for skin application and can be an effective dosage form for the treatment of Alopecia areata.

Design and Development of Propranolol Hydrochloride Transdermal Patches: In Vitro and Ex Vivo Characterization

2020 ◽  
Vol 3 (1) ◽  
pp. 01-08
Author(s):  
Chinthakindi Shravya
Keyword(s):  
Drug Release ◽  
Moisture Absorption ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Diffusion Mechanism ◽  
Propranolol Hydrochloride ◽  
Matrix Type ◽  
Transdermal Patches ◽  
Percent Moisture

The main aim of this investigation is to design and develop matrix type transdermal patches of Propranolol Hydrochloride which is an anti-hypertensive drug. These matrix type transdermal patches were prepared by “Solvent Casting Technique” using drug, HPMC E15 and Eudragit L 100 in the ratio of 1:6, 1:6.5, 1:7, 1:7.5, 1:8, 1:8.5, 1:9, 1:9.5. All formulations carried 20%v/w of PEG-600 as plasticizer. The prepared patches were characterized for various physicochemical parameters like weight, thickness, folding endurance, drug content, percent moisture content, percent moisture absorption, in vitro drug release and ex vivo permeation. Among this 1:9 ratio was found to be an Optimized formulation and patches were prepared by using permeation enhancers (lemon grass oil, Eucalyptus oil, and clove oil). The cumulative amount of drug release in 12hrs for F7 formulation showed maximum and used for that formulation skin permeation on Goat abdominal skin. FTIR studies show no interaction between drug, polymer and other excipients. The drug permeation kinetics followed “First order” and “zero order” profile with diffusion mechanism.

Development and Clinical Evaluation of Mucoadhesive Gastroretentive Tablets of Dipyridamole

2017 ◽  
Vol 10 (3) ◽  
pp. 3736-3744
Author(s):  
Kiran Kumar ◽  
Gurunath S ◽  
P Srikanth ◽  
Ajitha M ◽  
Y Madhusudan Rao
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Ex Vivo ◽  
Research Work ◽  
Storage Period ◽  
Physical Parameters ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets ◽  
The Stability

The present research work was focused to develop a mucoadhesive tablet dosage form for dipyridamole, which shows pH dependent solubility, it is highly soluble in acidic pH and as the pH increases the solubility of the drug decreases. Hence it was selected as the drug candidate for the present research. Mucoadhesive tablets of Dipyridamole were successfully prepared by using polymers like HPMC K4M, Chitosan and Isabgul husk by wet granulation method. FT-IR studies showed that there is no incompatibility between drug, polymer and various excipients used in the formulations. Formulated tablets have shown satisfactory results for physical parameters and complied with the pharmacopeial limits. The ex-vivo mucoadhesive strength and mucoadhesive force was found to be in the range of 16.15- 21.20 g and 1.56-2.06 N. Total ex-vivo mucoadhesive time was observed in between 10 to 12 hours. The in-vitro drug release was found to be more than 90% for the formulations FMD2, FMD3 and FMD8, up to 12 hours. Based on in-vitro drug release and mucoadhesive properties, formulation FMD2 was selected as optimized formulation. The dissolution data were further characterized by fitting the data into various kinetic models. The drug release from the matrices followed zero order with non-fickian release (diffusion + erosion controlled) for the optimized formulation. The optimized formulation was further subjected to swelling studies, which showed a swelling index of 286% up to 24 hours. The results indicated that the selected polymers were of swellable type. The stability studies were carried for 6 months as per ICH and WHO guidelines and the results of the stability study revealed that the optimized formulation is stable during the storage period. The in-vivo radiographic studies in fed condition, for the Mucoadhesive tablets (FMD2) showed a gastric residence time of more than 6 hours. When the radiographic images were taken at different time intervals and it was found to be in a particular location, which suggested that the retention of the dosage form might be due to the adhesion of dosage form to the gastric mucosa. 

Allopurinol Loaded Transferosomes for the Alleviation of Symptomatic After-effects of Gout: An Account of Pharmaceutical Implications

2020 ◽  
Vol 15 (4) ◽  
pp. 404-419
Author(s):  
Ruchi Tiwari ◽  
Gaurav Tiwari ◽  
Rachna Singh
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Skin Permeation ◽  
Skin Irritation ◽  
In Vivo Studies ◽  
Transdermal Drug Delivery System

Background: The present study assessed the transdermal potential of transferosomes loaded with allopurinol for the treatment of gout. Methods: Transferosomes of allopurinol were composed of different ratios of tween-80, soya lecithin and solvent using a thin-film hydration method. Transferosomes were characterized for Scanning Electron Microscopy (SEM), zeta potential, % entrapment efficiency (%EE), Fourier Transform Infrared Spectroscopy (FTIR), in-vitro drug release and kinetics as well as stability. Then, optimized formulation was incorporated in gel and evaluated for viscosity, pH, extrudability, homogeneity, skin irritation study, spreadability, ex vivo skin permeation study, flux, and stability. Results: SEM studies suggested that vesicles were spherical and zeta potential were in the range of -11.4 mV to -29.6 mV and %EE was 52.4- 83.87%. FTIR study revealed that there was no interaction between allopurinol and excipients during the preparation of transferosomes. The cumulative percentage of drug release from various transferosomes was ranged from 51.87 to 81.87%. A transferosomal gel of F8 formulation was prepared using dispersion method reported pseudoplastic rheological behavior, optimum pH, spreadability and maximum drug permeation i.e. 79.84% with flux 13.06 g/cm2/hr, followed zero-order release kinetics. Irritation and in-vivo studies of optimized transferosomal gel G8 on rabbits revealed better results than the standard allopurinol. Conclusion: This research suggested that allopurinol loaded transferosomal gel can be potentially used as a transdermal drug delivery system for the treatment of gout.

scholarly journals Evaluation of Transdermal Formulations of Metoclopramide Prepared Using Arachis Oil and Liquid Paraffin as Permeation Enhancers

2020 ◽  
Author(s):  
Sylvester O. Eraga ◽  
Matthew I. Arhewoh ◽  
Ogochukwu A. Meko
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Liquid Paraffin ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Tween 80 ◽  
Patient Acceptance ◽  
Scanning Calorimetry

Background: The study aimed to evaluate the effect of arachis oil and liquid paraffin on metoclopramide release from transdermal films. Objectives: Batches of metoclopramide films were prepared with hydroxypropyl methyl cellulose (HPMC), arachis oil or liquid paraffin and Tween 80 as plasticizer. The films were evaluated for their physiochemical properties, in vitro and ex vivo drug release and drug release kinetics. Drug-excipient interactions were investigated using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared (FTIR) spectroscopy. Methods: The transdermal films had a weight range of 0.22-0.24 g, folding endurance of 300-306, percentage moisture content and uptake of 2%-10% and 19%-110%, respectively and drug content of 98%-104%. There was similar condition in vitro release profile for the films but their ex vivo profiles exhibited variable drug release with the P3 (30% arachis oil) giving the highest drug (almost 100%) release.  Results: The release kinetics of metoclopramide followed the first order and Korsemeyer-Peppas models more closely as seen in their correlation coefficients (R2) of 0.9832 and 0.9560, respectively. Drug-excipient compatibility studies showed no interactions between excipients and metoclopramide. Conclusion: The formulated transdermal films showed controlled drug release over a period of 12 h. Arachis oil and liquid paraffin showed similar permeation enhancing ability. These enhanced permeation properties of the films could be helpful in the development of alternative route for metoclopramide administration in the management of emesis with improved patient acceptance.

The Development of Pemetrexed Diacid-Loaded Gelatin-Cloisite 30B (MMT) Nanocomposite for Improved Oral Efficacy Against Cancer: Characterization, In-Vitro and Ex-Vivo Assessment

2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Confocal Laser ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Cloisite 30B ◽  
Ft Ir

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.

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