Water-stable and finasteride-loaded polyvinyl alcohol nanofibrous particles with sustained drug release for improved prostatic artery embolization — In vitro and in vivo evaluation

The current study deals with the development and optimization of ispaghula (Plantago ovata F.) husk mucilage- (IHM-) alginate mucoadhesive beads containing glibenclamide by ionotropic gelation technique. The effects of sodium alginate (SA) to IHM and cross-linker (CaCl2) concentration on the drug encapsulation efficiency (DEE, %), as well as cumulative drug release after 10 hours (R10 h, %), were optimized using 32 factorial design based on response surface methodology. The observed responses were coincided well with the predicted values by the experimental design. The optimized mucoadhesive beads exhibited 94.43±4.80% w/w of DEE and good mucoadhesivity with the biological membrane in wash-off test and sustained drug release profile over 10 hours. The beads were also characterized by SEM and FTIR analyses. The in vitro drug release from these beads was followed by controlled release (zero-order) pattern with super case-II transport mechanism. The optimized glibenclamide-loaded IHM-alginate mucoadhesive beads showed significant antidiabetic effect in alloxan-induced diabetic rats over prolonged period after oral administration.

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High-amylose carboxymethyl starch matrices for oral sustained drug-release: In vitro and in vivo evaluation

European Journal of Pharmaceutics and Biopharmaceutics ◽

10.1016/j.ejpb.2006.12.001 ◽

2007 ◽

Vol 65 (3) ◽

pp. 371-378 ◽

Cited By ~ 35

Author(s):

T. Nabais ◽

F. Brouillet ◽

S. Kyriacos ◽

M. Mroueh ◽

P. Amores da Silva ◽

...

Keyword(s):

Drug Release ◽

Sustained Drug Release ◽

In Vivo Evaluation ◽

Carboxymethyl Starch ◽

Release In Vitro ◽

High Amylose

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Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.6.9 ◽

2017 ◽

Vol 10 (6) ◽

pp. 3929-3936

Author(s):

Y. Srinivasa Rao ◽

K. Adinarayana Reddy

Keyword(s):

Drug Release ◽

Patient Compliance ◽

Onset Of Action ◽

In Vivo Evaluation ◽

Disintegration Time ◽

In Vitro Drug Release ◽

Surface Ph ◽

Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

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

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.3.2 ◽

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.

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Synthesis, Characterization and in vivo Evaluation of PEGylated PPI Dendrimer for Safe and Prolonged Delivery of Insulin

Drug Delivery Letters ◽

10.2174/2210303109666190401231920 ◽

2019 ◽

Vol 9 (3) ◽

pp. 248-263 ◽

Cited By ~ 1

Author(s):

Ashish K. Parashar ◽

Preeti Patel ◽

Arun K. Gupta ◽

Neetesh K. Jain ◽

Balak Das Kurmi

Keyword(s):

Blood Glucose ◽

Drug Release ◽

Blood Glucose Level ◽

Glucose Level ◽

Albino Rats ◽

Sustained Delivery ◽

In Vivo Evaluation ◽

Hemolytic Toxicity

Background: The present study was aimed at developing and exploring the use of PEGylated Poly (propyleneimine) dendrimers for the delivery of an anti-diabetic drug, insulin. Methods: For this study, 4.0G PPI dendrimer was synthesized by successive Michael addition and exhaustive amidation reactions, using ethylenediamine as the core and acrylonitrile as the propagating agent. Two different activated PEG moieties were employed for PEGylation of PPI dendrimers. Various physicochemical and physiological parameters UV, IR, NMR, TEM, DSC, drug entrapment, drug release, hemolytic toxicity and blood glucose level studies of both PEGylated and non- PEGylated dendritic systems were determined and compared. Results: PEGylation of PPI dendrimers caused increased solubilization of insulin in the dendritic framework as well as in PEG layers, reduced drug release and hemolytic toxicity as well as increased therapeutic efficacy with reduced side effects of insulin. These systems were found to be suitable for sustained delivery of insulin by in vitro and blood glucose-level studies in albino rats, without producing any significant hematological disturbances. Conclusion: Thus, surface modification of PPI dendrimers with PEG molecules has been found to be a suitable approach to utilize it as a safe and effective nano-carrier for drug delivery.

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Synthesis and characterization of Chitosan-Catechol conjugates: Development and in vitro, in silico and in vivo evaluation of mucoadhesive pellets of lafutidine

Journal of Bioactive and Compatible Polymers ◽

10.1177/0883911521997849 ◽

2021 ◽

pp. 088391152199784

Author(s):

Loveleen Kaur ◽

Ajay Kumar Thakur ◽

Pradeep Kumar ◽

Inderbir Singh

Keyword(s):

Drug Release ◽

In Silico ◽

Ex Vivo ◽

Strong Interactions ◽

Dissolution Time ◽

Sem Images ◽

In Vivo Evaluation ◽

Release Studies

Present study was aimed to synthesize and characterize Chitosan-Catechol conjugates and to design and develop mucoadhesive pellets loaded with lafutidine. SEM images indicated the presence of fibrous structures responsible for enhanced mucoadhesive potential of Chitosan-Catechol conjugates. Thermodynamic stability and amorphous nature of conjugates was confirmed by DSC and XRD studies respectively. Rheological studies were used to evaluate polymer mucin interactions wherein strong interactions between Chitosan-Catechol conjugate and mucin was observed in comparison to pristine chitosan and mucin. The mucoadhesion potential of Chitosan-Catechol (Cht-C) versus Chitosan (Cht) was assessed in silico using molecular mechanics simulations and the results obtained were compared with the in vitro and ex vivo results. Cht-C/mucin demonstrated much higher energy stabilization (∆E ≈ −65 kcal/mol) as compared to Cht/mucin molecular complex. Lafutidine-loaded pellets were prepared from Chitosan (LPC) and Chitosan-Catechol conjugates (LPCC) and were evaluated for various physical properties viz. flow, circularity, roundness, friability, drug content, particle size and percent mucoadhesion. In vitro drug release studies on LPC and LPCC pellets were performed for computing t50%, t90% and mean dissolution time. The values of release exponent from Korsmeyer-Peppas model was reported to be 0.443 and 0.759 for LPC and LPCC pellets suggesting Fickian and non-Fickian mechanism representing drug release, respectively. In vivo results depicted significant controlled release and enhanced residence of the drug after being released from the chitosan-catechol coated pellets. Chitosan-Catechol conjugates were found to be a promising biooadhesive polymer for the development of various mucoadhesive formulations.

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Formulation development of folic acid conjugated PLGA nanoparticles for improved cytotoxicity of Caffeic acid phenethyl ester

Pharmaceutical Nanotechnology ◽

10.2174/2211738509666210111160528 ◽

2021 ◽

Vol 09 ◽

Author(s):

Harshad S Kapare ◽

Sathiyanarayanan L ◽

Arulmozhi S ◽

Kakasaheb Mahadik

Keyword(s):

Folic Acid ◽

Drug Release ◽

Caffeic Acid ◽

Caffeic Acid Phenethyl Ester ◽

Therapeutic Effects ◽

Formulation Development ◽

Sustained Drug Release ◽

Active Constituent

Background: Honey bee propolis is one of the natural product reported in various traditional systems of medicines including Ayurveda. Caffeic acid phenethyl ester (CAPE) is an active constituent of propolis which is well known for its anticancer potential. The therapeutic effects of CAPE are restricted owing to its less aqueous solubility and low bioavailability. Objective: In this study CAPE loaded folic acid conjugated nanoparticle system (CLFPN) was investigated to enhance solubility, achieve sustained drug release and improved cytotoxicity of CAPE. Methods: Formulation development, characterization and optimization were carried out by design of experiment approach. In vitro and in vivo cytotoxicity study was carried out for optimized formulations. Results: Developed nanoparticles showed particle size and encapsulation efficiency of 170 ± 2 - 195 ± 3 nm and 75.66 ± 1.52 - 78.80 ± 1.25 % respectively. Optimized formulation CLFPN showed sustained drug release over a period of 42 h. GI50 concentration was decreased by 46.09% for formulation as compared to CAPE in MCF-7 cells indicating targeting effect of CLFPN. An improved in vitro cytotoxic effect was reflected in in-vivo Daltons Ascites Lymphoma model by reducing tumor cells count. Conclusion: The desired nanoparticle characteristic with improved in vivo and in vitro cytotoxicity was shown by developed formulation. Thus it can be further investigated for biomedical applications.

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DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

Journal of Biomedical and Pharmaceutical Research ◽

10.32553/jbpr.v7i6.559 ◽

2018 ◽

Vol 7 (6) ◽

Author(s):

Mohini Sihare ◽

Rajendra Chouksey

Keyword(s):

Drug Release ◽

Release Kinetics ◽

In Vitro Release ◽

Release Profile ◽

Matrix Tablets ◽

In Vivo Studies ◽

Release Mechanism ◽

In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

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Design and evaluation of a novel floating osmotic pump system

Journal of Pharmacy & Pharmaceutical Sciences ◽

10.18433/j33k5n ◽

2009 ◽

Vol 12 (1) ◽

pp. 129 ◽

Cited By ~ 3

Author(s):

Zhihong Zhang ◽

Bo Peng ◽

Xinggang Yang ◽

Chao Wang ◽

Guangmei Sun ◽

...

Keyword(s):

Drug Release ◽

Oral Administration ◽

In Vitro Release ◽

Osmotic Pump ◽

Matrix Tablets ◽

In Vivo Evaluation ◽

Pump System ◽

Conventional Tablet

PURPOSE. Find a novel delivery system for oral administration of drugs that have absorption window in the upper part of gastrointestinal (GI) track. METHODS. Dipyridamole was chosen as the model drug. A novel system, which combined the osmotic pump controlled release system and the floating system, was designed; matrix tablets (MT) were prepared for compares. The effects of pH, temperature and hydrodynamic conditions on drug release and the floating behavior of floating osmotic pump system (FOP) were investigated. In vivo evaluation was performed by a three-crossover study in six Beagle dogs relative to the conventional tablet (CT). Cumulative percent input in vivo was compared with that of in vitro release profiles. RESULTS. Floating behavior of FOP, drug releases from FOP and MT were sensitive to pH of dissolution media but not sensitive to temperature; the release of dipyridamole from MT was influenced by stirring rate while drug release from FOP was not. AUC of FOP was larger than MT and CT. The linear correlations between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP-a true zero-order release formula, whereas only a nonlinear correlation was obtained for MT. CONCLUTIONS. FOP could be a novel way for the oral administration for drugs like dipyridamole.

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Design Optimization and In Vitro-In Vivo Evaluation of Orally Dissolving Strips of Clobazam

Journal of Drug Delivery ◽

10.1155/2014/392783 ◽

2014 ◽

Vol 2014 ◽

pp. 1-15 ◽

Cited By ~ 8

Author(s):

Rajni Bala ◽

Sushil Khanna ◽

Pravin Pawar

Keyword(s):

Tensile Strength ◽

Drug Release ◽

Content Uniformity ◽

In Vivo Evaluation ◽

Disintegration Time ◽

Significant Difference ◽

Film Formulation ◽

Test Film

Clobazam orally dissolving strips were prepared by solvent casting method. A full 32 factorial design was applied for optimization using different concentration of film forming polymer and disintegrating agent as independent variable and disintegration time, % cumulative drug release, and tensile strength as dependent variable. In addition the prepared films were also evaluated for surface pH, folding endurance, and content uniformity. The optimized film formulation showing the maximum in vitro drug release, satisfactory in vitro disintegration time, and tensile strength was selected for bioavailability study and compared with a reference marketed product (frisium5 tablets) in rabbits. Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm2), and in vitro drug release (96.6%). Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product. The mean ratio values (test/reference) of Cmax (95.87%), tmax (71.42%), AUC0−t (98.125%), and AUC0−∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.

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