scholarly journals EFFECT PROCESSING VARIABLES ON THE CHARACTERISTICS OF ITRACONAZOLE HOLLOW MICROSPHERES

2019 ◽  
pp. 108-115
Author(s):  
SURBHI ROHILLA ◽  
D. C. BHATT ◽  
SHAVETA AHALWAT
Keyword(s):  
Drug Release ◽  
Spherical Surface ◽  
Entrapment Efficiency ◽  
Storage Conditions ◽  
Physicochemical Analysis ◽  
Stability Study ◽  
Hollow Microspheres ◽  
Release Mechanism ◽  
Low Density

Objective: The purpose of the study was to develop the multiple unit non-effervescent gastroretentive floating hollow microspheres to enhance the bioavailability of the drug by varying the concentration of low-density polymer and release modifier to retaining the formulation at its absorption site. Design of experiment approach applied to get the best possible formulation with minimum assets and experimentation. Methods: The hollow microspheres were prepared by emulsion solvent diffusion-evaporation technique using ethylcellulose as low-density polymer and Eudragit E100 as release modifier. The central composite design was used for the optimization of independent variables and was evaluated for particle size, entrapment efficiency, in vitro floating ability and drug release characteristics. Results: The physicochemical analysis was done to confirm any interaction between drug and excipients. The Scanning Electron Microscopy (SEM) showed a smooth, spherical surface with an inner hollow cavity. The stability study proves that the hollow microspheres were more stable under different storage conditions with no significant changes in formulation. The drug release mechanism of the optimized batch can be explained by Korsmeyer Peppas model. Conclusion: Based on the results, the hollow microspheres with a release modifying polymer offers a superior approach to retain the formulation in the stomach.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

DESIGN, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE NASAL IN SITU GELLING FORMULATIONS OF VENLAFAXINE HYDROCHLORIDE FOR BRAIN TARGETTING

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 25-31
Author(s):  
M Priyanka ◽  
◽  
F. S. Dasankoppa ◽  
H. N Sholapur ◽  
NGN Swamy ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Linear Regression Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Drug Content ◽  
Venlafaxine Hydrochloride ◽  
In Situ Gelling

The poor bioavailability and the therapeutic effectiveness exhibited by the anti-depressant venlafaxine hydrochloride on oral administration is overcome by the use of ion-activated gel forming systems that are instilled as drops; these undergo gelation in the nasal cavity. The present study describes the design, characterization and evaluation of mucoadhesive nasal in situ gelling drug delivery of venlafaxine hydrochloride using different polymers like sodium alginate, HPMC and pectin in various concentrations. DSC studies revealed compatibility of the drug and excipients used. The in situ gels were characterized for physicochemical parameters, gelling ability, rheological studies, drug content, drug entrapment efficiency, in vitro mucoadhesive strength, water holding capacity, gel expansion coefficient and in vitro drug release studies. The amount of polymer blends was optimized using 23 full factorial design. The influence of experimental factors on percentage cumulative drug release at the end of 2 and 8 hours were investigated to get optimized formulation. The responses were analyzed using ANOVA and polynomial equation was generated for each response using multiple linear regression analysis. Optimized formulation, F9, containing 1.98% w/V sodium alginate, 0.64% w/V hydroxylpropyl methylcellulose, 0.99% w/V pectin showed percentage cumulative drug release of 19.33 and 80.44 at the end of 2 and 8 hours, respectively, which were close to the predicted values. The optimized formulation was subjected to stability study for three months at 300C /75% RH. The stability study revealed no significant change in pH, drug content and viscosity. Thus, venlafaxine hydrochloride nasal mucoadhesive in situ gel could be successfully formulated to improve bioavailability and to target the brain.

scholarly journals Design, Development and Evaluation Of Anti-Hypertensive Drug Solid Lipid Nano Particles

2021 ◽  
Vol 11 (4) ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Entrapment Efficiency ◽  
Nano Particles ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solid Lipid ◽  
Wide Range

Recently, solid lipid Nano-particles have received much attention by the researchers owing to its biodegradability, biocompatibility and the ability to deliver a wide range of drugs. The aim of the present study was to design Diltiazem solid lipid Nano-particles and to evaluate them. Diltiazem solid lipid Nano-particles were prepared by hot homogenization technique using different lipids (Tristearin, GMS and Comprital), soy lecithin as stabilizers and tween 80, Poloxamer as surfactants. The Nano-particles were evaluated for particle size & PDI, zeta potential, entrapment efficiency and in vitro drug release. The particle size ranged from 49.7 to 523.7 nm. PDI of all formulations were good within the range of 0.189 to 0.427. The zeta potential ranged from -10.5 to -29.6 Mv, Entrapment efficiency of all formulations were observed was in the range of 78.68 to 95.23 %. The cumulative percentage release of Diltiazem from different Diltiazem Nano-particles varied from 53.36 to 88.74% depending upon the drug lipid ratio and the type of lipid used. The average percentage of drug released from different SLNs after 24 hours showed in the following order: F9 (53.35%) < F6 (56.75%) < F4 (61.74%) < F7 (63.8%) < F5(67.77%) < F8(69.04%) < F3(75.31%) < F1(79.36%) <F2 (88.74%) respectively. The release kinetic studies showed that the release was first order diffusion controlled and the n values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Quasi-Fickian type (n-value of 0.47). Keywords: Diltiazem, solid lipid Nano-particles, FTIR, in vitro drug release.

scholarly journals Formulation and evaluation of nanoparticulate ofloxacin ophthalmic gel using ionic gelation method

2019 ◽  
Vol 1 (2) ◽  
pp. 73-78
Author(s):  
B Syed Salman ◽  
Mohd Abdul Hannan Baig
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Entrapment Efficiency ◽  
Release Mechanism ◽  
Ionic Gelation ◽  
In Vitro Drug Release ◽  
Entire Study ◽  
Drug Content ◽  
Higuchi Model

Oflaxacin is an ophthalmic and topical anti-bacterial agent used in the management of Allergic conjunctivitis, Trachoma, Blepharitis. The basic idea behind the development of such a system is to maintain a sustained drug release from the dosage form. Oflaxacin is suitable candidate for formulation into sustained dosage form in order to prolong the release of drug. The drug-excipient compatibility studies were carried out by using FTIR technique. Based on the results, excipients were found to be compatible with ofloxacin. In preformulation study, estimation of Ofloxacin was carried out by systronics UV spectrophotometer at λmax 284nm using distilled water, which had a good reproducibility and this method was used in entire study. Formulation was prepared by using ionic gelation method .The response drug content, entrapment efficiency, diffusion, spreadability, In vitro drug release was evaluated Drug content ranging from to 82.6 % to 91.24% entrapment efficiency values are ranged from 91.25% to 94.02% and in -vitro drug release studies are also studied. The In-vitro drug release study of Ofloxacin was carried out by using In-vitro diffusion apparatus.100ml of using tear fluid was taken in a beaker. The solution was stirred with 100rpm by maintaining the temperature of 37˚c ± 5˚c. The drug release data were explored for this type of release mechanism followed. The best fit with the highest determination R2 coefficients was shown by both the models (zero and peppas) followed by Higuchi model which indicate the drug release via diffusion mechanism. However as indicated by the values of R both of the models (zero and peppas) followed by Higuchi model were found to be efficient in describing the release of Ofloxacin.

scholarly journals FORMULATION AND EVALUATION OF ELASTIC LIPOSOMES OF DECITABINE PREPARED BY ROTARY EVAPORATION METHOD

2019 ◽  
Author(s):  
Nwobodo Ndubuisi Nwobodo ◽  
Adamude Fatima Amin ◽  
Dingwoke Emeka John ◽  
Abraham Ubhenin
Keyword(s):  
Drug Release ◽  
Dna Methyltransferase ◽  
Entrapment Efficiency ◽  
Skin Penetration ◽  
Topical Administration ◽  
Systemic Circulation ◽  
Stability Study ◽  
Evaporation Method ◽  
Rotary Evaporation

Decitabine is a cytidine deoxynucleoside analog, which acts by inhibiting DNA methyltransferase, and is used for the treatment of acute myeloid leukemia. Decitabine has a short half-life (25 minutes), and is sensitive to harsh conditions. Elastic liposomes are an effective tool that can be used to overcome this disadvantage. Elastic liposomes also known as transfersomes are modified lipid carriers that enable drug to reach deeper skin layers and/or the systemic circulation. These vesicular formulations are several orders of magnitudes, more deformable than the standard liposomes and thus well suited for skin penetration. The objective of present study is to develop and evaluate the elastic liposomes of Decitabine so as to provide the sustained release and improve its bioavailability. Elastic liposomes were prepared by rotary evaporation method using Span 80 and Span 60 as a surfactants. The prepared Elastic liposomes were evaluated for entrapment efficiency, vesicle size, in vitro drug release. The drug release profiles from different elastic liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. Based on different parameters formulations of batch ELS1 was found to be the best formulations. Stability study was performed on the selected formulation ELS1. Study concludes that Decitabine can also be formulated in the liposomal carrier which finds its best way for the topical administration.

scholarly journals Development and Characterization of Elastic Liposomes of Metronidazole for the Treatment of Bacterial Infection

2020 ◽  
Vol 10 (6-s) ◽  
pp. 83-88
Author(s):  
Priyam Chaurasiya ◽  
Ritesh Agarwal ◽  
Kavita R. Loksh
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Stability Study ◽  
Vesicle Size ◽  
Rotary Evaporation ◽  
Span 60

Objective: The objective of present study is to develop and evaluate the elastic liposomes of metronidazole so as to provide the sustained release and improve its bioavailability. Methods: Elastic liposomes were prepared by rotary evaporation method using Span 80 and Span 60 as a surfactants. The prepared elastic liposomes were evaluated for entrapment efficiency, vesicle size, In vitro drug release. Results: The drug release profiles from different elastic liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. The formulation prepared showed an average vesicle size 185.4nm. The amount of drug entrapped into the elastic liposomes formulations was determined. The entrapment efficiency was found to be 73.45±0.78 %. A good amount of drug was entrapped in the liposome formulations prepared. Based on different parameters formulations of batch TG2 was found to be the best formulations. Stability study was performed on the selected formulation TG2. When the regression coefficient values of were compared, it was observed that ‘r’ values of first order was maximum i.e. 0.993 hence indicating drug release from formulations was found to follow Korsmeyer Peppas model release kinetics Conclusion: These results indicate that elastic liposome can function as probable drug delivery systems to enhance transdermal permeation of metronidazole for treating the topical infections. Keywords: Metronidazole, Elastic liposomes, Topical administration, Skin infection

Etoposide-Loaded Microparticles Prepared with Poly (Hydroxybutyrate-Co-Hydroxyvalerate) and Poly(-Caprolactone) Blends: Formulation, Characterization and in vitro Drug Release

1970 ◽  
Vol 1 (3) ◽  
pp. 251-256
Author(s):  
Patel J. K ◽  
Tank H. M
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Release Mechanism ◽  
Evaporation Process ◽  
In Vitro Drug Release ◽  
Drug Release Mechanism ◽  
Drug Entrapment Efficiency ◽  
Solvent Evaporation Process ◽  
Poly Caprolactone

The purpose of this research was to formulate and systematically evaluate etoposide-loaded microparticles. Etoposide microparticles containing poly(hydroxybutyrate-co-hydroxyvalerate) and poly(-caprolactone) were prepared by an emulsion/solvent evaporation process. Microparticles were discrete, spherical and free flowing. The microparticles showed high % of yeild and drug entrapment efficiency. Etoposide-loaded microparticles demonstrated drug sustained releases (up to 200 hours). The drug release mechanism was dependent on the presence of PCL in the microparticles. The release of etoposide caused an increase in the surface area of the microparticles. A Fickian release was determined for the microparticles prepared exclusively with P(HBHV), while non-Fickian release behaviors were found for the P(HBHV)/PCL microparticles.

scholarly journals HESPERIDIN HYDROGEL FORMULATION USING PECTIN-CHITOSAN POLYMER COMBINATION

2017 ◽  
Vol 9 (12) ◽  
pp. 98 ◽  
Author(s):  
Andhi Fahrurroji ◽  
Dea Thendriani ◽  
Hafrizal Riza
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
The Body ◽  
Flavonoid Glycosides ◽  
Release Mechanism ◽  
Factorial Method ◽  
Optimum Formula ◽  
Therapy Target

Objective: Hesperidin is flavonoid glycosides that proven to have therapeutic activity to any desease, one of them is colon disease; but, its low solubility (< 100 mg/L) makes small absosption inside the body so it needs delivery system that could deliver hesperidin to the therapy target. The objective of this research is to get optimum formula from hydrogel with polimer pectin-chitosan combination that can control in vitro hesperidin release.Method: Optimum hydrogel formula determination using Design Expert 7.0.0 with factorial method design, resulted in formula plans with pectin-chitosan consentration comparison of (P3% : C1%), (P3% : C2%), (P5% : C1%), (P5% : C2%) respectively.Result: Optimum formula with pectin : chitosan concentration comparison (5% : 1%) has entrapment efficiency about 96.658%; k(/hour) swelling index at pH 5.0, 6.8, and 7.4, about 34.917, 15.766, and 8.146 respectively; drug release at pH 5.0, 6.8, and a medium contained 2% mouse’s caecum  about 0.461, 20.116, and 52.955% respectively; and the mucoadhesive strength about 0.184 N/cm2.Conclusion: The combination of pectin-chitosan polymer in hydrogel muchoadhesive matrix can control hesperidin in vitro release with the drug release value at the highest concentration of pectin in medium contained 2% mouse’s saecum that could release drug about 56%. Hesperidin hydrogel release mechanism follows Higuchi kinetic.

scholarly journals RATIONAL DESIGNING OF SUSTAINED RELEASE MATRIX FORMULATION OF ETODOLAC EMPLOYING HYPROMELLOSE, CARBOMER, EUDRAGIT AND POVIDONE

2017 ◽  
Vol 9 (12) ◽  
pp. 92
Author(s):  
Nilesh N. Mahajan ◽  
Pooja Wadhavane ◽  
Debarshi Kar Mahapatra
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Stability Study ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Toxic Substances ◽  
Drug Release Profile ◽  
Matrix Formulation

Objective: The existing investigation represents a challenge in formulating etodolac oral controlled release tablets employing five most prominent hydrophilic release rate retardant polymers like HPMC K100M, HPMC K4M, Carbopol 934P, Eudragit RS100, and Polyvinyl pyrrolidone K90 which are USFDA approved non-toxic substances, cost-effective, and easily available.Methods: The tablets were manufactured by wet granulation method along with talc, anhydrous lactose, and magnesium stearate. The pre-compression attributes of the produced granules and the post-compression characteristics were assessed according to the specified protocols. The formulations were accessed for their ability to release the drug in the simulated gastric media and the obtained results were fitted into various kinetic models to determine the probable drug release mechanism(s). A short-term stability study (for 90 days duration) was also performed.Results: The prepared granules demonstrated superior flow properties and packing ability, whereas the fabricated sustained release matrix batches showed excellent mechanical characteristics. The in vitro drug release profile of the hypromellose, carbomer, eudragit and povidone based sustained release matrix tablet formulations expressed drug release for the period of 12 hr following the diffusion cum erosion mechanism(s) (termed as anomalous diffusion) and illustrated comparable drug release with that of marketed formulation (Etogesic®-ER 600 mg). The produced formulations revealed splendid reproducibility and stability under accelerated conditions.Conclusion: The judiciously planned fabrication of the matrix formulations possess the ability to decrease the frequency of drug administration to twice-daily along with minimizing the blood level fluctuations, which ultimately leads to enhanced patient compliance and better therapeutic regimens.

scholarly journals Design and Evaluation of Microspheres Loaded With Pirenzepine

2018 ◽  
Vol 10 (02) ◽  
Author(s):  
A. Aparna ◽  
C. M. Shalina ◽  
D.V.R.N. Bhikshapathi
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Calcium Chloride ◽  
Entrapment Efficiency ◽  
Oral Route ◽  
Cross Linking ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Ich Guidelines

The current objective of the investigation was to fabricate Pirenzepine loaded microspheres for the treatment of gastritis delivered through oral route. The microspheres were prepared by ionotropic gelation technique using sodium as alginate polymer and calcium chloride as cross-linking agent. The effect of polymer and cross-linking agent on particle size, shape, % yield, entrapment efficiency, and drug release were studied. The prepared microspheres morphology and physicochemical properties of were investigated by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Among the total S14 formulations, S7 formulation was optimized at 2.2% of sodium alginate, 7% of calcium chloride maintained100rpm for 10 min at room temperature. The optimized S7 formulation displayed the %EE 94.10%, particle size 82.45 ± 0.09μm, % yield 96.30% and swelling index of 95.13%. From In vitro drug release studies S7 shown 97.17 ± 0.28% up to 12 h in 0.1N HCl, and the drug release followed the zero order and Korsmeyer- Peppas model (R2 = 0.987, 0.995) respectively, indicating the possible drug release mechanism to be by erosion and diffusion. The marketed product showed the drug release of 95.23 ± 0.21% within 1 h. The optimized S7 formulation subjected to stability studies for 6months as per ICH guidelines, no appreciable difference was observed hence the S7 formulation found stable. The data obtained thus suggest that a micro particulate system can be successfully designed for sustained delivery of Pirenzepine and to improve its bioavailability

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