scholarly journals Formulation and evaluation of Acyclovir microparticles for Ocular Delivery

2016 ◽  
Vol 4 (2) ◽  
pp. 41-51
Author(s):  
Shekhar Singh ◽  
Anil Middha ◽  
Randhir Singh Dahiya
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Zeta Potential ◽  
Ethyl Cellulose ◽  
Ocular Delivery ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Sustained Drug Delivery ◽  
Evaporation Technique

The objective of the present work was to formulate and evaluate microparticles of Acyclovir and produced sustained drug delivery for ocular delivery. In this 9 batches(A1-C3) of acyclovir microparticle was prepared with ethyl cellulose, PVA and other ingredients by solvent evaporation technique. The prepared microparticles were evaluated for different parameters i.e % Drug yield, % Drug entrapment, Surface morphology, Zeta potential and in-vitro drug release for 24hrs in phosphate buffer 7.4 and simulated tear fluid. The best batch was performed stability studies for 6 months. The research concluded that Acyclovir microparticles could be a alternative for conventional dosage formand other phytochemical in herbs.

scholarly journals PREPARATION, CHARACTERIZATION AND EVALUATION OF FLOATING MICROPARTICLES OF CIPROFLOXACIN

2016 ◽  
Vol 9 (1) ◽  
pp. 1 ◽  
Author(s):  
Sumit Durgapal ◽  
Sayantan Mukhopadhyay ◽  
Laxmi Goswami
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Evaluation Parameters

Objective: The main purpose of this study is to prepare a floating micro articulated drug delivery system of ciprofloxacin by using non-aqueous solvent evaporation technique to increase the bioavailability and therapeutic effectiveness of the drug by prolonging its gastric residence time.Methods: Floating microparticles were prepared by using different low-density polymers such as ethyl cellulose and hydroxypropyl methylcellulose either alone or in combination with the aid of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as percentage yield, drug content, drug entrapment, rheological studies, floating characteristics and in vitro drug release studies.Results: Drug-excipient compatibility studies performed with the help of FTIR instrument indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique is a suitable technique for the preparation of floating microspheres as most of the formulations were discrete and spherical in shape with a good yield of 65% to 85% and 15 to 22 h of floating duration with 90% of maximum percentage floating capacity shown by formulation FM9. Though, different drug-polymer ratios, as well as a combination of polymers, play a significant role in the variation of overall characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, drug content, drug entrapment, rheological studies and in vitro drug release characteristics formulation FM9 was found to fulfil the criteria of ideal floating drug delivery system.Conclusion: Floating microparticles were successfully prepared, and from this study, it can be concluded that the developed floating microspheres of ciprofloxacin can be used for prolonged drug release in the stomach to improve the bioavailability and patient compliance.

scholarly journals FORMULATION AND EVALUATION OF FLOATING MATRIX TABLETS OF LEVOFLOXACIN HEMIHYDRATE USING HYDROXYPROPYL METHYLCELLULOSE K4M TO TREAT HELICOBACTER PYLORI INFECTION

2018 ◽  
Vol 11 (6) ◽  
pp. 148
Author(s):  
Srinivasa Rao Baratam ◽  
Vijayaratna J
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Linear Regression Method ◽  
In Vitro Drug Release ◽  
Sustained Drug Delivery

Objective: The aim of the study was to develop a floating drug delivery system of levofloxacin (LVF) hemihydrate for sustained drug delivery to improve the extended retention in the stomach, oral bioavailability, and local site-specific action in the stomach. Methods: Preparation of LVF tablets using melt granulation method using hydroxypropyl methylcellulose (HPMC) K4M with sodium bicarbonate as gas generating agent. From LFTA1 to LFTA5, formulations were developed and evaluated for floating properties for swelling characteristics and in vitro drug release studies. In vitro dissolution was carried out using USP II paddle method using 0.1N HCI pH buffer at 50 rpm and samples were measured at 294 nm using ultraviolet-visible spectroscopy. Results: Obtained Fourier-transform infrared charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. In vitro drug release was performed and drug release kinetics were evaluated using the linear regression method and were found to be followed the zero-order release by diffusion controlled release. Optimized formula was found to be LFTA4 with 20% of a polymer with 99.03% of drug release with 12 h of floating time and 32 s floating lag time. Conclusion: Matrix tablets (LFTA4) formulated employing 20% HPMC K4M are best suited to be used for gastroretentive dosage form of LVF.

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 and Characterization of Ondansetron Hydrochloride Matrix Tablets for Sustained Drug Delivery

2019 ◽  
Vol 11 (04) ◽  
Author(s):  
P Gupta ◽  
V A Sethi ◽  
A W Siddiqui ◽  
L K Tyagi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Ethyl Cellulose ◽  
Extended Period ◽  
Matrix Tablets ◽  
In Vitro Drug Release ◽  
Ondansetron Hydrochloride ◽  
Release Study

The objective of proposed work was to develop Ondansetron Hydrochloride (OND HCl) sustained release matrix tablets for the better treatment of vomiting for extended period of time. Sustained release matrix tablet is the drug delivery system that is designed to achieve a prolonged therapeutic effect by continuously releasing medication over an extended period of time after administration of single dose. The matrix tablets of OND HCl were prepared by direct compression method using varying ratio of hydroxy propyl methyl cellulose (HPMC) and ethyl cellulose. The bends of tablets were evaluated for bulk and tapped density, % compressibility index and angle of repose and powder of all formulations blend exhibited that low interparticle friction and excellent flow characteristics. The prepared matrix tablets were then assessed for different physical tests like consistency of weight, thickness, hardness, friability, drug content and in vitro drug release. Each batch of the OND HCl matrix tablets were of good quality as to hardness, thickness, friability and % medicament content. The in vitro drug release study was done for 2 hours by utilizing paddle technique in 0.1N HCl (pH 1.2) as dissolution media and 6 hours using phosphate buffer (pH 6.8) as dissolution media. The drug release study showed that all formulation FMT-1, FMT-2, FMT-3, FMT-4, FMT-5 and FMT-6 were provide the drug release on sustained manner up to 8 hrs. Amongst the developed matrix tablets formulations, FMT-2 containing ethyl cellulose (100 mg) was optimized as best because FMT-2 show highest drug release profile and promoting the sustained release of drug, which could potentially improve the patient compliance.

scholarly journals FORMULATION DEVELOPMENT OF ACYCLOVIR MICROSPHERE USING NOVEL NATURAL POLYMER

2018 ◽  
Vol 8 (5-s) ◽  
pp. 271-276
Author(s):  
Priyanka Singh ◽  
Shailendra K Lariya
Keyword(s):  
Drug Release ◽  
Antiviral Agent ◽  
Polydispersity Index ◽  
Natural Polymer ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Sustained Drug Delivery ◽  
Evaporation Technique ◽  
Plasma Half Life

Acyclovir [9-(2-hydroxyethoxymethyl) guanine] is an acyclic nucleoside analogue of guanosine that is a potent and selective antiviral agent. It has a relatively short plasma half-life (3 hr). When orally administered, it is slowly and scarcely absorbed from the gastrointestinal tract. The objective of the present work was to formulate and evaluate microspheres of Acyclovir and produced sustained drug delivery. In these 14 batches of acyclovir microspheres was prepared with using natural polymer Kondagogu gum and other ingredients by solvent evaporation technique. The prepared microspheres were evaluated for different parameters i.e % Drug yield, % drug entrapment, shape, surface morphology, particles size, polydispersity index, zeta potential and in-vitro drug release for 48 hrs in phosphate buffer 7.4. The best batch was performed stability studies for 6 months. The research concluded that Acyclovir microspheres could be an alternative for conventional dosage form and other phytochemical in herbs. Keywords: Acyclovir, Microspheres, Kondagogu gum, Polydispersity index, in-vitro drug release

scholarly journals FORMULATION AND IN VIVO EVALUATION OF SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM OF RAMIPRIL IN WISTAR RATS

2021 ◽  
pp. 126-136
Author(s):  
NALLAPU JAYAPAL ◽  
YAMSANI VAMSHI VISHNU
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Systemic Absorption ◽  
Content Uniformity ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Pure Drug

Objective: The aim was to formulate and evaluate self-nanoemulsifying drug delivery systems (SNEDDS) of ramipril, an antihypertensive drug to improve the solubility and bioavailability. Methods: Based on solubility studies oil phase (Sefsol 218), surfactant (Acrysol EL135), and cosurfactant (Transcutol P), respectively, were selected to prepare SNEDDS. Ramipril SNEDDS optimized employing box-Behnken design through the study of factors. All formulations were evaluated for particle size, zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE), drug content, and in vitro drug release. The optimized formulation was characterized for Fourier transform infrared (FTIR), scanning electron microscopy (SEM), stability studies, and pharmacokinetic study. Results: The mean particle size, PDI, ZP, EE, content uniformity, and in vitro drug release profile of optimized ramipril-loaded SNEDDS (RF14) were found to be 75.3±2.21nm, 0.126±0.05, −24.4±5.78mV, 98.74±1.97%, 99.52±1.67%, and 98.65±1.73%, respectively. FTIR studies revealed that there is no incompatibility between drug and excipients, SEM images exhibited nanoparticles to be more porous and in spherical shape. Stability studies indicated formulation was stable for 6 months. In vivo studies were conducted for optimized formulation RF14, the Tmax was found to be 0.5±0.62 and 0.5±0.95 h for the optimized and commercial formulations respectively, while Cmax was 25.16±1.73 ng/mL was significant (p<0.05) as compared to the ramipril pure drug 8.02±0.086 ng/mL. AUC0-t of the SNEDDS formulation was higher 355.49±1.76ng h/ml compared to pure drug 116.57±1.64 ng h/ml indicated higher amount of drug concentration in blood proving better systemic absorption of ramipril from SNEDDS formulation as compared to the pure drug. Conclusion: It is concluded from the results that ramipril was successfully formulated into SNEDDS with higher concentration with fast action.

scholarly journals DEVELOPMENT AND EVALUATION OF NOVEL DRUG DELIVERY SYSTEM OF TOLTERODINE TARTRATE

2017 ◽  
Vol 9 (5) ◽  
pp. 29 ◽  
Author(s):  
Vijaykumar Patil ◽  
Deepak Belsare
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Accelerated Stability ◽  
Tolterodine Tartrate ◽  
Novel Drug Delivery System ◽  
Novel Drug

Objective: Tolterodine tartrate (tolterodine) is used for treating overactive bladder (OAB) with symptoms of urinary frequency, urgency and leakage. Tolterodine is an antimuscarinic (anticholinergic) agent. It works by blocking a chemical that causes contractions of the bladder. Present work involved development of a novel drug delivery system of tolterodine intended to be taken once daily.Methods: Extended release (ER) pellets of tolterodine were prepared and optimized for in vitro drug release. Subsequently, these pellets were filled into a suitable sized capsule. The resulting capsules were evaluated for in vitro drug release. Optimized formulation was subjected to accelerated stability studies for 3 mo and was evaluated for description, average weight, assay and drug release.Results: The optimized ER capsule exhibited similar dissolution profile as that of the reference listed drug (RLD), with approximately 45%, 75% and more than 80% release in 3 h, 5 h and 7 h respectively. Accelerated stability studies indicated good physical and chemical stability of the formulation.Conclusion: ER formulation of tolterodine was optimized and can be used as once a day dosage, reducing the frequency of administration when compared with the immediate release formulation. The developed formulation exhibited similar behavior as that of reference formulation Detrol LA marketed in the US.

Development and Characterization of Acetazolamide Nanoemulsion for Effective Ocular Delivery

2021 ◽  
Vol 11 (5) ◽  
Author(s):  
Joshi Neha ◽  
Juyal Vijay ◽  
Arya Rajeshwar K.K. ◽  
Joshi Himanshu
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Phase Diagrams ◽  
Delivery System ◽  
Tween 20 ◽  
Ocular Delivery ◽  
In Vitro Drug Release ◽  
Ternary Phase Diagrams ◽  
Droplet Sizes

Nanoemulsion has the potential of releasing the drug continuously, and they may easily permeate via the intense layers of the eye structure due to nano-size droplets, which makes nanoemulsion an effective drug delivery system for ocular delivery. The objective of our work was to prepare a nanoemulsion of acetazolamide for glaucoma treatment with enhanced efficacy as well as for continuous effect. Based on different compositions of oil (Olive Oil), surfactants (Tween-20), and co-surfactants (Transcutol P), forty-five test mixtures were made, water titration technique was employed for preparing the pseudo-ternary-phase diagrams. On the basis of these phase diagrams, twenty-five acetazolamide loaded nanoemulsion were formulated and examined for their nanosized droplets, PDI, zeta potential, viscosity, pH, transmittance and in-vitro drug release. The formulated nanoemulsion showed all the properties within the desired range i.e., droplet size (15.6 to 21.18), zeta potential (-15.5 to- 24.71), PDI (0.140 to 0.361), viscosity (3.234 ± 0.063to 5.174 ± 0.023cps), pH (6.922 ± 0.026to 7.033 ± 0.012), RI (1.379 ± 0.007 to 1.404 ± 0.006) and % transmittance was found (94.96± 0.6% to 96.68± 0.6%) and also the release rate of acetazolamide from nanoemulsion was found very good i.e., 81.59± 1.04% to 92.46± 0.33% after 24 hrs. The top four formulations having good drug release were selected for further evaluation of droplet sizes and which also fall in the nano range (15.68 to 21.18 nm). The study showed that it is possible to develop nanoemulsion of phenytoin drug, and the in-vitro drug release study showed that the prepared nanoemulsion had good bioavailability, sustained release and ability to target eye as an effective ocular delivery system.

scholarly journals DESIGN AND EVALUATION OF INTRAGASTRIC BUOYANT TABLETS OF VENLAFAXINE HYDROCHLORIDE

2017 ◽  
Vol 10 (5) ◽  
pp. 166
Author(s):  
Parasuram Rajam Radhika ◽  
Nishala N ◽  
Kiruthika M ◽  
Sree Iswarya S
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Xanthan Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Methyl Cellulose ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Floating Drug Delivery ◽  
Venlafaxine Hydrochloride

Objective: The present study was undertaken to prolong the release of orally administered drug. The aim is to formulate, develop, and evaluate theintragastric buoyant tablets of venlafaxine hydrochloride, which releases the drug in a sustained manner over a period of 12 hrs. Different formulationswere formulated using the polymers Carbopol 934 P, xanthan gum, hydroxypropyl methylcellulose (HPMC K100M) with varying concentration ofdrug: Polymer ratio of 1:1, 1:1.5, 1:2, in which sodium bicarbonate acts as gas generating agent, and microcrystalline cellulose as a diluent.Methods: The tablets were prepared by direct compression and evaluated for tablet thickness, weight variation, tablet hardness, friability, in vitrobuoyancy test, in vitro drug release and Fourier transform infrared spectroscopy. Formulations were evaluated by floating time, floating lag time and in vitro drug release. Dissolution profiles were subjected for various kinetic treatments to analyze the release pattern of drug.Results: It was found that drug release depends on swelling, erosion, and diffusion, thus following the non-Fickian/anomalous type of diffusion.Formulation F8 was considered as an optimized formulation for gastro retentive floating tablet of venlafaxine hydrochloride. The optimizedformulation showed sustained drug release and remained buoyant on the surface of the medium for more than 12 hrs. As the concentration of HPMCK100M increases in the formulation the drug release rate was found to be decreased. The optimized formulation was subjected for the stability studiesand was found to be stable as no significant change was observed in various evaluated parameters of the formulation.Conclusion: It can be concluded that floating drug delivery system of venlafaxine hydrochloride can be successfully formulated as an approach toincrease gastric residence time, thereby improving its bioavailability.Keywords: Venlafaxine hydrochloride, Intragastric buoyant, Floating drug delivery systems, Hydroxypropyl methyl cellulose K100M, Carbopol 934 P,Xanthan gum.

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