Biodegradable Solid Lipid Microparticles Loaded With Diltiazem Hydrochloride for Oral Delivery: Preparation and in-Vitro/in-Vivo Evaluation

Pilaniya, Urmila

doi:10.22270/jddt.v1i1.10

Cited by 6 publications

(5 citation statements)

References 15 publications

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“…The DSC data of the SLMs showed that the melting peaks as well as the enthalpies depend on the PEG and drug contents of the formulations. The physico-chemical compatibility of the drug and the excipients studied by DSC suggested an absence of drug incompatibility, consistent with similar studies (Jaspart et al, 2005;Long et al, 2006;Eradel et al, 2009;Pilaniya et al, 2011). The results revealed the compatibility of gentamicin and the excipients as well as the stability of the drug in the lipid matrix.…”

Section: Discussionsupporting

confidence: 89%

“…Since drug-loaded SLMs formulations containing highest amount of drug (i.e. 3% w/w gentamicin) especially batch C 3 gave the highest permeation flux and coefficient, it implies that sustained release gentamicin dosage form might be developed with this formulation, consistent with some drug-loaded SLMs formulations (Jaspart et al, 2005;Long et al, 2006;Eradel et al, 2009;Pilaniya et al, 2011). Generally, batches C 1 -C 3 gave greater permeation fluxes and coefficients than corresponding batches B 1 -B 3 and A 1 -A 3 SLMs formulations.…”

Section: Discussionmentioning

confidence: 71%

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Solid lipid micro-dispersions (SLMs) based on PEGylated solidified reverse micellar solutions (SRMS): a novel carrier system for gentamicin

Kenechukwu¹,

Momoh²,

Nnamani³

et al. 2014

Drug Delivery

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The purpose of this study was to formulate and evaluate novel PEGylated solidified reverse micellar solutions (SRMS)-based solid lipid microparticles (SLMs) for improved delivery of gentamicin. Lipid matrix (SRMS) [consisting of 15% w/w Phospholipon® 90G (P90G) in 35% w/w dika wax (Irvingia gabonensis) was formulated and characterized by differential scanning calorimetry (DSC). SLMs were formulated by melt-emulsification using the SRMS, PEG 4000 and gentamicin (1.0, 2.0, 3.0% w/w), and their physicochemical as well as pharmacokinetic parameters determined. In vitro permeation of gentamicin from the SLMs through artificial membrane (0.22 μm pore size) was carried out using Franz's cell and phosphate-buffered saline (PBS, pH 7.4) as acceptor medium, while bioevaluation was performed using clinical isolates of Pseudomonas aeruginosa and Staphylococcus aureus. Stable and irregularly-shaped gentamicin-loaded SLMs of size range 34.49 ± 2.56 to 53.52 ± 3.09 µm were obtained. The SLMs showed sustained drug permeation and exhibited time-dependent and capacity-limited bioactivity. Overall, SLMs containing 2% w/w SRMS, 3% w/w gentamicin and PEG 4000 entrapped the highest amount of drug, gave highest IZD against the test organisms and highest permeation flux (5.239 μg/cm(2).min) and permeation coefficient (1.781 × 10(-6)cm/min) within 420 min, while pure gentamicin gave the least. Preliminary in vivo pharmacokinetic studies also showed an AUC-24 of 1507 µg/h/ml for the optimized formulation, while that of oral drug solution was 678 µg/h/ml. This showed a 2.2-fold increase in the systemic bioavailability of gentamicin from the optimized formulation. PEGylated SRMS-based SLMs prepared with heterolipid from Irvingia gabonensis would likely offer a reliable delivery system for gentamicin.

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Section: Discussionsupporting

confidence: 89%

Section: Discussionmentioning

confidence: 71%

Solid lipid micro-dispersions (SLMs) based on PEGylated solidified reverse micellar solutions (SRMS): a novel carrier system for gentamicin

Kenechukwu¹,

Momoh²,

Nnamani³

et al. 2014

Drug Delivery

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“…Overall medication release from the polymer matrix may be reduced as a result of this effect. 32 At the conclusion of the 24-hr period, zidovudine release from the SLM ranged from 70.47 percent to 100 percent. SLM 8 was able to achieve the needed 80 percent medication release for the best therapeutic concentration.…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

Utility of Different Lipids and Effect of Soya Lecithin on Sustained Delivery of Zidovudine via Biodegradable Solid Lipid Microparticles: Formulation and in-vitro Characterization

Sathyamoorthy¹,

Sundar²,

Rajendran³

et al. 2022

IJPER

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Background: Zidovudine (Azidothymidine, AZT) is widely used in the treatment of Acquired Immuno Deficiency Syndrome (AIDS) and related conditions, either alone or in combination with other antiviral agents to combat HIV. AZT is a Biopharmaceutical Classification System (BCS) class III drug and has various disadvantages. Thus, AZT is a potential candidate for delivery via lipid-based drug delivery system. Materials and Methods: In the present work, solid lipid microparticles (SLMs) of Zidovudine were developed for sustaining the drug release, to overcome or to reduce the hepatic metabolism and to ensure optimal bioavailability. A total of sixteen formulations of Zidovudine loaded solid lipid microparticles in two groups viz., one with tripalmitin and another with trimyristin were prepared by emulsion-solvent evaporation method. Results: The average particle size and entrapment efficiency of the prepared SLM varied between 5.48 µm-10.64 µm and 46.92 % and 58.39% respectively. The release of zidovudine from the SLM varied between 70.47% and 100% at the end of 24 hrs. 80% of the drug release which is required for obtaining the optimal therapeutic concentration was achieved by SLM 8. Conclusion: Formulation SLM 8 was considered best with maximum sustainability in the drug release along with maintaining therapeutic optimum. The formulation was found stable under stressed conditions.

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“…Solid lipid microparticles were irstly developed in 1990 and are considered a promising drug carrier system, especially for the introduction of the active drug substance and to carry and inally release for controlled drug delivery (Pilaniya et al, 2011). The spherical microparticles of lipid with a size range of 1-1000µm can be suspended in a suitable aqueous solvent system offer possible new ways to develop an improved new therapeutic product (Ojha, 2014).…”

Section: Introductionmentioning

confidence: 99%

Formulation Design and Evaluation of Solid Lipid Micro-particles of Curcumin for the Treatment of Alzheimer’s disease

Mir¹,

Ashraf²,

Mahmud³

2020

ijrps

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Solid lipid microparticles reach the site of its action in a controlled rate and do show controlled release for a better therapeutic result. A good drug carrying and release system involve a controlled drug delivery that improves bioavailability, to enrich stability and to minimise the toxic effects followed with a targeted drug at the site of its action. The solid lipid microparticles of curcumin were prepared in a view to achieving high permeability of curcumin in the brain through blood-brain-barrier. The lipid microsphere solids were prepared by hot melts microencapsulation technique to formulate solid lipid microspheres. Twelve lipid formulations were prepared with varying concentration of surfactants (span 40, span 70, span 90 and Tween 100). The developed formulation was subjected to various parameters such as the particle size, % entrapment efficiencies, yield productions, % cumulative release, percentage yield and drug loading, based upon highest entrapment efficiency, drug release and % cumulative release, the F3 formulation was considered as the best formulation. The prepared microsphere was subjected to different evaluation parameters such as thin-layer chromatography, melting point, FTIR, solubility, compatibility study and In-vitro drug release. The developed formulation shows spherical and smooth surface. The percentage release of drug F3 formulation has been found highest of about 86.23% after 12 hr.

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Biodegradable Solid Lipid Microparticles Loaded With Diltiazem Hydrochloride for Oral Delivery: Preparation and in-Vitro/in-Vivo Evaluation

Cited by 6 publications

References 15 publications

Solid lipid micro-dispersions (SLMs) based on PEGylated solidified reverse micellar solutions (SRMS): a novel carrier system for gentamicin

Solid lipid micro-dispersions (SLMs) based on PEGylated solidified reverse micellar solutions (SRMS): a novel carrier system for gentamicin

Utility of Different Lipids and Effect of Soya Lecithin on Sustained Delivery of Zidovudine via Biodegradable Solid Lipid Microparticles: Formulation and in-vitro Characterization

Formulation Design and Evaluation of Solid Lipid Micro-particles of Curcumin for the Treatment of Alzheimer’s disease

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