scholarly journals CURCUMIN LOADED POLYMERIC MICROSPHERES FOR VAGINAL DELIVERY: FORMULATION DESIGN, IN VITRO EVALUATION, KINETICS AND STABILITY STUDIES

2021 ◽  
Vol 10 (2) ◽  
pp. 56-60
Author(s):  
J Adlin Jino Nesalin ◽  
Shafiya Khanum
Keyword(s):  
Drug Release ◽  
Vaginal Delivery ◽  
Delivery System ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Vaginal Gel

The main objective of this research is to evaluate a new approach for the preparation of bio adhesive microparticles and to design an innovative vaginal delivery system for curcumin which is able to enhance the drug anticancer activity. Curcumin encapsulated microspheres were prepared by solvent evaporation method. The microspheres were found to be discrete, spherical with free-flowing properties and evaluated for particle size analysis, shape (scanning electron microscopy), drug encapsulation efficiency, FTIR, DSC studies and in vitro release performance. The best selected microsphere formulation (F2, containing drug: polymer ratio 1:2) was incorporated into gels with a bio adhesive polymer. The microencapsulated vaginal gels were evaluated for pH, spreadability, extrudability, viscosity, in vitro drug release, drug release kinetics, bio adhesion test, accelerated stability of selected gel formulation. In vitro drug release rate for selected microencapsulated bio adhesive vaginal gel (FS3 gel, containing 1 % w/w of drug loaded microspheres and 0.6 % w/w of Carbopol 934) was found to sustain curcumin over 12h. The results were then compared statistically and obtained a satisfactory correlation. Thus, in conclusion preparation protocol of microencapsulated vaginal gel study may be adopted for a successful development of newer drug delivery system of other drugs for administration to vagina.

scholarly journals CURCUMIN LOADED CHITOSAN NANOPARTICLES FOR TOPICAL DELIVERY: FORMULATION DESIGN, IN VITRO EVALUATION, KINETICS AND STABILITY STUDIES

2021 ◽  
Vol 10 (2) ◽  
pp. 48-52
Author(s):  
J Adlin Jino Nesalin ◽  
Preethi Raj M N
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Topical Delivery ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Topical Gel

The main objective of this research is to evaluate a new approach for the preparation of bio adhesive nanoparticles and to design an innovative topical delivery system for curcumin which is able to enhance the drug anticancer activity. Curcumin encapsulated nanoparticles were prepared by ionic gelation method. The nanoparticles were found to be discrete, spherical with free-flowing properties and evaluated for particle size analysis, shape (scanning electron microscopy), drug encapsulation efficiency, FTIR, DSC studies and in vitro release performance. The best selected nanoparticles formulation (FS5, containing drug: polymer ratio 1:5) was incorporated into gels with a bio adhesive polymer. The Nanoencapsulated topical gels were evaluated for pH, spreadability, extrudability, viscosity, in vitro drug release, drug release kinetics, bio adhesion test, accelerated stability of selected gel formulation. In vitro drug release rate for selected Nanoencapsulated bio adhesive topical gel (FS3 gel, containing 1 % w/w of drug loaded nanoparticles and 0.6 % w/w of Carbopol 934) was found to control curcumin release over 12h. The results were then compared statistically and obtained a satisfactory correlation. Thus, in conclusion preparation protocol of Nanoencapsulated topical gel study may be adopted for a successful delivery of Curcumin for topical use.

Formulation and Evaluation of Transdermal patch of Methimazole

2021 ◽  
pp. 4667-4672
Author(s):  
Nani Tadhi ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Transdermal Patch ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Percent Moisture ◽  
Release Study

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.

Fabrication and Release Kinetics of Liposomes Containing Leuprolide Acetate

2021 ◽  
Vol 7 (1) ◽  
pp. 35-38
Author(s):  
Sudipta Das ◽  
Arnab Samanta ◽  
Koushik Bankura ◽  
Debatri Roy ◽  
Amit Nayak
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Zero Order ◽  
Leuprolide Acetate ◽  
Lipid Film ◽  
In Vitro Drug Release ◽  
Liposomal Formulations ◽  
Kinetics Of

The present work is focused on the preparation and in vitro release kinetics of liposomal formulation of Leuprolide Acetate. In this work, “Thin Lipid Film Hydration Method” was used for preparation of Leuprolide Acetate loaded liposomes. Prepared liposomal formulations of Leuprolide acetate was evaluated by drug entrapment study, in-vitro drug release kinetics and stability studies. The percentage drug entrapment of Leuprolide acetate for F1 and F2 formulations were found to be 78.14 ± 0.67 and 66.70 ± 0.81% respectively. In-vitro drug release study of liposomal formulations had shown zero order release pattern. Regression co-efficient (R2) value of Zero order kinetics for F1 and F2 formulations were 0.9912 and 0.9676 respectively. After storing formulations for 1 month, stability testing was done at 40C.It was found that all batches were stable. These liposomal formulations of Leuprolide acetate can be formulated for parenteral application to treat prostate cancer and in women, to treat symptoms of endometriosis (overgrowth of uterine lining outside of the uterus) or uterine fibroids.

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 PREPARATION AND CHARACTERIZATION OF SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ANTI-HYPERTENSIVE DRUG’’

2020 ◽  
Vol 9 (4) ◽  
Author(s):  
Anukumar E ◽  
Nagaraja T S ◽  
Yogananda R ◽  
Bharathi D R
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Release Kinetics ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Hypertensive Drug

The present work is to prepare and characterization of self nano emulsifying drug delivery system containing Anti-hypertensive drug. Losartan is a competitive antagonist and inverse agonist of angiotensin 2 receptor. The SNEDDS is prepared by Sonication method using a components of SPAN 60/Eudragit RS 100 as a surfactant, PVA as a Co-surfactant, Iso propyl alcohol as a solvent and DCM as a co-solvent. The prepared SNEDDS was evaluated for Fourier transform infrared spectroscopy, Surface morphology, particle size, zeta potential,  drug entrapment efficiency, visual assessment, self-emulsification time, Robustness to dilution, in-vitro drug release and short term stability studies. The in-vitro drug release data of all the formulations were found to be zero order over a period of 24 h and Formulation F7 shows good results for the drug release kinetics as controlled release. The stability studies data was found that there was no such difference in drug EE and in-vitro drug release.

scholarly journals Formulation Development and Characterisation of Gemifloxacin Mesylate and Loteprednol Etabonate Ophthalmic Ocuserts

2020 ◽  
Vol 11 (2) ◽  
pp. 2549-2557
Author(s):  
Swati Mayur Keny ◽  
Ketan Shah
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
In Vitro Release ◽  
Antibacterial Drug ◽  
Formulation Development ◽  
Loteprednol Etabonate ◽  
In Vitro Drug Release ◽  
Solvent Cast ◽  
Release Study

Gemifloxacin Mesylate is a fluoroquinolone antibacterial drug preferably used in the treatment of bacterial conjunctivitis. The addition of Loteprednol Etabonate enhances the anti-inflammatory activity of the developed formulation. The objective of the present work was to develop ocular inserts of Gemifloxacin Mesylate with Loteprednol Etabonate and thereby evaluate its potential as a sustained ocular delivery system. Poor bioavailability and poor therapeutic responses are associated with conventional ophthalmic solutions due to many pre-corneal constraints. These constrain trigger the researcher's mind to formulate a controlled and sustained drug delivery system. Ocular inserts based on the solvent cast technique were formulated and characterized by in vitro drug release studies using a flow-through apparatus that simulated the eye conditions. Compatibility of Gemifloxacin Mesylate, Loteprednol Etabonate, polymer, and excipients was checked based on preformulation studies. Different combinations of Gemifloxacin Mesylate, Loteprednol Etabonate, Carbopol 974, 98 981, PEG 400, and glycerine were formulated by the solvent cast method and evaluated. Clarity, smoothness, surface pH, drug content, and in-vitro drug release study were the various parameters evaluated on the formulated ocusert. Formula GLE 74 fulfilled the needs of all organoleptic parameters and also the in-vitro release study. Based on in vitro correlation stability studies, it was concluded that this ocular inserts formulation could be a promising controlled release formulation.

Development and Evaluation of Floating Tablets of Lamivudine

2021 ◽  
pp. 2593-2597
Author(s):  
Chinmaya Keshari Sahoo ◽  
Amiyakanta Mishra ◽  
Amaresh Prusty ◽  
S. Ram Mohan Rao ◽  
Jimidi Bhaskar
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Stability Study ◽  
Compression Method ◽  
Short Term ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Vitro Release

The present study was undertaken to develop floating tablets of lamivudine. The tablets were prepared by direct compression method. The prepared tablets were evaluated for pre compression parameters, post compression parameters, in vitro drug release study and in vitro buoyancy study. Among the prepared formulations F4 batch show 90.98% drug release in 12 h. The in vitro release kinetics were analyzed for different batches by different pharmacokinetic models such as zero order, first order, Higuchi, and Korsmeyer Peppas. The result of optimized formulation releases drug up to 12 h in a controlled manner and follows Higuchi kinetics. Short term stability study at 40±2ºC/75±5% RH for three months on the best formulation was performed showing no significant changes in thickness, hardness, friability, drug content and in vitro drug release.

scholarly journals Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal Candidiasis

2013 ◽  
Vol 63 (3) ◽  
pp. 359-372 ◽  
Author(s):  
Naresh Vishal Gupta ◽  
Shirodker Natasha ◽  
Anil Getyala ◽  
Ramnath Sudeendra Bhat
Keyword(s):  
Drug Release ◽  
Chemical Interaction ◽  
Drug Loading ◽  
Particle Size Analysis ◽  
Vaginal Candidiasis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Dsc Studies

Abstract The aim of the present investigation was to prepare and evaluate novel bioadhesive vaginal tablets containing clotrimazole loaded microspheres in order to provide long-term therapeutic activity at the site of infection. Tablets were prepared by incorporating drug loaded microspheres and using bioadhesive polymers hydroxypropylmethylcellulose, sodium carboxymethylcellulose and Carbopol. Microspheres were prepared by the spray drying technique using Eudragit RS-100 and Eudragit RL-100. Microspheres were characterized by SEM, DSC, FTIR, particle size analysis and evaluated for percentage yield, drug loading, encapsulation efficiency and in vitro drug release. To achieve bioadhesion to the mucosal tissue, optimized microspheres were incorporated into bioadhesive tablets and were evaluated for in vitro drug release, in vitro and in vivo mucoadhesion. FTIR and DSC studies showed that no chemical interaction occurred between the drug and polymers. The sphericity factor indicated that the prepared microspheres were spherical. Formulation Mt6 indicated a controlled in vitro drug release and good bioadhesive strength. The in vivo images confirmed the bioadhesion and retention property of tablets up to 24 h. The results indicated that this drug delivery system can be explored for controlled intravaginal drug release.

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED-RELEASE PELLETS OF LORNOXICAM

2021 ◽  
pp. 221-227
Author(s):  
MILIND J. AMIN ◽  
KEYUR S. PATEL ◽  
DEEPA R. PATEL ◽  
ZIL P. PATEL ◽  
JAYANTI V. BAJAG
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Compatibility Study ◽  
In Vitro Drug Release ◽  
Dependent Variables ◽  
Full Factorial ◽  
Eudragit Rlpo

Objective: The aim of the study was to develop sustained release pellets of lornoxicam using Eudragit RLPO and Eudragit RSPO to reduce the dosing frequency. Methods: The sustained release pellets of lornoxicam were prepared by extrusion–spheronization technique using Eudragit RLPO and Eudragit RSPO as release retardant polymers and microcrystalline cellulose as spheronizing agent. A 32 Full factorial design was applied to investigate the combined effect of the two independent variables i.e. concentration of Eudragit RLPO (X1) and concentration of Eudragit RSPO (X2) on the dependent variables, In vitro drug release at 1h (Y1), In vitro drug release at 4 h (Y2) and In vitro drug release at 12 h. (Y3). Results: The optimized formulation (F0) show in vitro drug release 11.24±1.21 %, 43.69±1.28 %, 82.69±1.74 % and 100.24±1.56 % at 1 h, 4 h, 12 h and 24 h respectively. Drug excipients compatibility study by FTIR showed no interaction between drug and excipients. Eudragit RLPO and Eudragit RSPO had a significant effect on in vitro drug release. Conclusion: From all parameters and experimental design evaluation, it was concluded that the drug release rate decreased with an increase the concentration of Eudragit RLPO and Eudragit RSPO. SEM Photomicrograph of pellets revealed that the surface was rough and the pellets were spherical shaped in nature. The in vitro release kinetics revealed higuchi model is followed and drug release is by anamolous diffusion.

scholarly journals Mucoadhesive microspheres based formulation development of ziprasidone hydrochloride for nasal delivery

2020 ◽  
Vol 10 (5) ◽  
pp. 175-181
Author(s):  
Yogita Sahu ◽  
Sourabh Jain ◽  
Karunakar Shukla
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Research Work ◽  
In Vitro Release ◽  
Nasal Delivery ◽  
Size Analysis ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Chitosan Microspheres

The purpose of research work was to develop and optimize mucoadhesive microspheres of Ziprasidone hydrochloride for nasal delivery with the aim to enhance the residence time and improve therapeutic efficacy. Mucoadhesive drug delivery systems are those that provide intimate contact of the drug with the mucosa for an extended period of time. In our present work, mucoadhesive chitosan microspheres were prepared by emulsification method using liquid paraffin as external phase. Ten different formulations were developed. Results show that as the concentration of polymer increases it affects the particle size, production yield, encapsulation efficiency, swelling index, in-vitro mucoadhesion and in-vitro drug release of mucoadhesive microspheres. The in vitro mucoadhesion of microspheres was investigated using freshly isolated goat nasal mucosa. The mucoadhesion for M0, M1, M2, and M9 was tested. The mucoadhesion property was satisfactory. The M2 exhibited lowest mucoadhesion of 68.9%, and M0 displayed highest mucoadhesion of 87.5%. The In Vitro release studies it revealed that 84.1% of drug release from formulation M1 at 7hrs. The 50% of the drug was released from the formulation M2 and 70.67% from formulation M9.This formulations were further used for SEM for particles size analysis, mucoadhesion test and in-vitro drug release. The In-vitro % drug release data suggest that the maximum and sustained drug release was obtained for formulation M1.The present study showed that Ziprasidone hydrochloride chitosan microspheres can deliver intanasally which can improve the therapeutic outcome for the Epileptic seizure. Keywords: Ziprasidone hydrochloride, Mucoadhesive microspheres, Nasal drug delivery, Drug Entrapment efficiency.

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