Formulation of sustained-release microspheres of cefixime with enhanced oral bioavailability and antibacterial potential

Aim: The present work focused on the development of sustained-release microsphere formulation of cefixime to provide reduction in dosing frequency, improved antibacterial activity and patient compliance. Methodology & results: Microspheres were prepared by modified emulsion solvent evaporation method and evaluated by in vitro and in vivo studies. Optimized formulation (FK-07) was found to have entrapment efficiency of 81.12 ± 0.93% and particle size of 166.82 ± 0.86 μm. FK-07 sustained release up to 24 h as demonstrated by in vitro drug release and in vivo pharmacokinetic study in rats. FK-07 showed approximately twofold increase in bioavailability and twofold decrease in MIC90 value against Escherichia coli, Klebsiella pneumoniae and Salmonella typhi in comparison to marketed formulation. Conclusion: Sustaining the release of cefixime using microspheres enhanced its bioavailability, antibacterial efficacy and will help in reducing its dosing frequency.

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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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Formulation and Evaluation of Meloxicam In-Situ Gel Designed for Sustained Drug Release to Reduce Dosing Frequency in the Management of Arthritis

International Journal of Pharmaceutical Sciences Review and Research ◽

10.47583/ijpsrr.2021.v69i02.025 ◽

2021 ◽

Vol 69 (2) ◽

Author(s):

Meesala. Srinivasa Rao ◽

M. S Chandra Goud ◽

C. V. Reddy

Keyword(s):

Drug Release ◽

Sustained Release ◽

Sustained Drug Release ◽

In Vitro Drug Release ◽

In Situ Gel ◽

Dosing Frequency ◽

Gel Formulations

Meloxicam has short biological half-life and is rapidly eliminated, frequent oral administration is necessary to maintain its therapeutic concentration, but this can increase chances of missing dose. This makes Meloxicam a good applicant for oral sustained release formulation. The objective of study was to develop in-situ gel formulations of Meloxicam for sustained release to reduce the dosing frequency in the treatment of rheumatoid arthritis. Method of Ion sensitive in-situ gelation was used in this study. Meloxicam In-situ gel formulations were prepared by varying concentrations of sodium alginate as a bio-degradable gel forming polymer, CaCl2 as a cross-linking agent and Chitosan/ HPMCK4/HPMCK15/Guar gum/Gellan gum/ Xantha gum/pectin were used as drug release rate controlling polymers. The formulations F11-F18 were assessed for Physical appearance, pH, in-vitro drug release, viscosity, in-vitro gelling capacity and drug content. FTIR, DSC and in-vivo drug kinetics studies was conducted for Meloxicam, excipients used and optimized formulation. Formulations showed an optimum viscosity that will allow ease of administration and swallowing. All formulations are shown pH between4.7-4.9, floating lag time was 2-3sec and floated for >12 hrs. In vitro drug release studies reporting that commercially available product Meloxicam SR has showed 99.92% drug release in 8 hrs and out of eight formulations F11 showing in-vitro drug release of 99.52% over a 12hrs extended period. FTIR studies revealed no interaction between drug and excipients used. The results of In-vivo kinetic studies are approving the better performance of the optimized formulation in comparison to marketed formulation, The Cmax, Tmax, half-life AUC values are confirming the same thing. In conclusion, Formulation (F11) was selected as optimized formulations could be offered as shows optimum sustained drug release compared to commercial formulation. Hence Meloxicam containing Chitosan as drug release controll

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In vitro and in vivo Evaluation of Pramipexole HCl Mucoadhesive Microspheres

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2018.100509 ◽

2018 ◽

Vol 10 (05) ◽

Author(s):

K. Subbarao ◽

G. Suresh

Keyword(s):

Drug Delivery ◽

Entrapment Efficiency ◽

In Vivo Studies ◽

The Novel ◽

In Vivo Evaluation ◽

In Vitro Drug Release ◽

Efficient Management ◽

Gastro Retentive

The study was aimed to design and develop the novel gastro retentive mucoadhesive Pramipexole microspheres using ionotropic gelation technique. Based on the results of Micromeretic properties confirmed that microspheres were free flowing with good pack ability. The optimized M13 formulation displayed the % entrapment efficiency 96.07%, % yield 98.01%, swelling index 96.08% and Mucoadhesiveness was 95.42%. The in vitro drug release showed the sustained release of Pramipexole up to 99.16 ± 5.12% within 12 h. FTIR studies revealed incompatibility was not found between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M13) 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-∞ and t1/2 were calculated. The marketed product Cmax (2.19 ± 0.01 ng/ml) was higher than optimized formulation (2.0 ± 0.01 ng/ml). The optimized formulation AUC0-t (20.15 ± 1.12 ng.hr/ml), AUC0-∞ (27.42 ± 1.16 ng.hr/ml) was significantly higher than that of marketed product AUC0-t (13.21 ± 1.26 ng.hr/ml) and AUC0-∞ (19.15 ± 1.13 ng.hr/ml) respectively. Which indicated the optimized formulation bioavailability was higher than marketed product. Microspheres would be a promising drug delivery system which plays potentially significant role in pharmaceutical drug delivery in the efficient management of Parkinson’s disease.

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Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2013.6.4.10 ◽

2013 ◽

Vol 6 (4) ◽

pp. 2269-2280

Author(s):

Nagratna Dhople ◽

P N Dandag ◽

A P Gadad ◽

C K Pandey ◽

Masthiholimath V S

Keyword(s):

Sustained Release ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Sustained Release Formulation ◽

Prokinetic Drug ◽

Drug Entrapment Efficiency ◽

Itopride Hydrochloride ◽

Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

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Development of In Situ Self-Assembly Nanoparticles to Encapsulate Lopinavir and Ritonavir for Long-Acting Subcutaneous Injection

Pharmaceutics ◽

10.3390/pharmaceutics13060904 ◽

2021 ◽

Vol 13 (6) ◽

pp. 904

Author(s):

Irin Tanaudommongkon ◽

Asama Tanaudommongkon ◽

Xiaowei Dong

Keyword(s):

Sustained Release ◽

Trough Concentration ◽

Self Assembly ◽

Subcutaneous Injection ◽

Drug Loading ◽

Entrapment Efficiency ◽

Long Acting

Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses. Here, a long-acting subcutaneous injection of lopinavir (LPV) in combination with ritonavir (RTV) using in situ self-assembly nanoparticles (ISNPs) was developed to potentially overcome adherence barriers. The ISNP approach can improve the pharmacokinetic profiles of the drugs. The ISNPs were characterized in terms of particle size, drug entrapment efficiency, drug loading, in vitro release study, and in vivo pharmacokinetic study. LPV/RTV ISNPs were 167.8 nm in size, with a polydispersity index of less than 0.35. The entrapment efficiency was over 98% for both LPV and RTV, with drug loadings of 25% LPV and 6.3% RTV. A slow release rate of LPV was observed at about 20% on day 5, followed by a sustained release beyond 14 days. RTV released faster than LPV in the first 5 days and slower than LPV thereafter. LPV trough concentration remained above 160 ng/mL and RTV trough concentration was above 50 ng/mL after 6 days with one subcutaneous injection. Overall, the ISNP-based LPV/RTV injection showed sustained release profiles in both in vitro and in vivo studies.

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Rifapentine Polylactic Acid Sustained-Release Microsphere Complex for Spinal Tuberculosis Therapy: Preparation, in vitro and in vivo Studies

Infection and Drug Resistance ◽

10.2147/idr.s304864 ◽

2021 ◽

Vol Volume 14 ◽

pp. 1781-1794

Author(s):

Zhen Wang ◽

Abulikemu Maimaitiaili ◽

Tengfei Wang ◽

Xinghua Song

Keyword(s):

Sustained Release ◽

Polylactic Acid ◽

Spinal Tuberculosis ◽

In Vivo Studies ◽

Tuberculosis Therapy

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Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2019/v31i630356 ◽

2019 ◽

pp. 1-8

Author(s):

Marwa H. Abdallah ◽

Amr S. Abu Lila ◽

Md. Khalid Anwer ◽

El-Sayed Khafagy ◽

Muqtader Mohammad ◽

...

Keyword(s):

Drug Release ◽

Zeta Potential ◽

Drug Loading ◽

Entrapment Efficiency ◽

Tween 80 ◽

Formulation Development ◽

In Vitro Drug Release ◽

Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

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DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i3.23145 ◽

2018 ◽

Vol 11 (3) ◽

pp. 284

Author(s):

Pravin S Patil ◽

Shashikant C Dhawale

Keyword(s):

Particle Size ◽

Drug Release ◽

Dissolution Rate ◽

Drug Carrier ◽

Entrapment Efficiency ◽

Significant Rise ◽

Scanning Calorimetry ◽

In Vitro Drug Release

Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

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