Formulation and Evaluation of Floating Polymeric Nanoparticles of Linagliptin in Capsules

Prasanthi, D; Kumari, J Krishna; Hymavathi, S

doi:10.5530/jyp.2020.12s.43

Cited by 3 publications

(3 citation statements)

References 3 publications

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“…Several techniques have been adopted to increase LIN bioavailability, like the incorporation into floating polymeric nanoparticles [4], solid lipid nanoparticles [5], SMEDDS [6], niosomes [7], eudragit coated sensitive SLN [8], as well as employment of natural phenols such as gallic and ellagic acid [9] and nanospsheres [10].…”

Section: Fig 1 Structure Of Linagliptin (Lin)mentioning

confidence: 99%

Development of Linagliptin Ultra Fine Solid Supersaturated Bio-SNEDDS Using Triangular Mixture Design for Enhancement of Oral Bioavailability: Impact of P-gp Inhibition

Mansour,

El-Gawad,

Boughdady

2023

J. Pharm. Res. Int.

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Linagliptin (LIN) is a newly developed dipeptidyl peptidase 4 (DPP-4) inhibitor oral antidiabetic drug. LIN is considered a P-gp substrate, thus suffers from poor bioavailability (< 30%). The aim of this study was to develop and characterize LIN bioactive self-nanoemulsifying drug delivery system to circumvent its poor bioavailability and enhance its therapeutic efficacy. Methodology: In this study, we developed solid supersaturated bioactive self-nanoemulsifying drug delivery system (Ss-bio-SNEDDS) of LIN, using clove oil as an oil phase, cremophor CO 40 as a surfactant, labrasol as a co-surfactant and Hydroxy-propyl-B-cyclodextrin (HPBCD) as a precipitation inhibitor (PI); all components are of established P-gp inhibition activity. Optimization was performed by means of triangular mixture design based on particle size, poly dispersity index (PDI) and percent transmittance. The two optimized formulations (F4 and F8) were designated and evaluated for stability and cloud point. Also, the effect of pH on particle size and PDI was assessed. Additionally, examination of particles’ surface morphology of the two optimized formulations was performed by transmission electron microscope (TEM). The prepared liquid supersaturated-SNEDDS (s-SNEDDS) were converted into solid supersaturated-SNEDDS (Ss-SNEDDS) via adsorption on microcrystalline cellulose (MCC). Further evaluations were carried out, including in vitro drug release, in vitro precipitation and in vivo studies. Results: The optimized formulations F4 and F8 manifested promising characteristics concerning particle size (< 50 nm), PDI (< 0.3) and percent transmittance (> 99%). Stability study showed no phase separation or precipitation with rapid emulsification time. The two optimized formulations showed high cloud point temperature (above 70°C). TEM images of F4 and F8 showed spheroid like appearance with relatively smooth surface. Results of the in vivo study in rats revealed a significant increase in AUC of solid-F4, solid-F8 and solid supersaturated-F4 (S-F4, S-F8 and Ss-F4) by 2.32, 2.89 and 2.54 folds, respectively compared to LIN solution; with a noticeable reduction in blood glucose level at each point. Conclusion: In a nutshell, Ss-bio-SNEDDS are considered as auspicious nano-carriers for LIN with the virtue of augmented bioavailability and possible dose reduction.

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Section: Fig 1 Structure Of Linagliptin (Lin)mentioning

confidence: 99%

Development of Linagliptin Ultra Fine Solid Supersaturated Bio-SNEDDS Using Triangular Mixture Design for Enhancement of Oral Bioavailability: Impact of P-gp Inhibition

Mansour,

El-Gawad,

Boughdady

2023

J. Pharm. Res. Int.

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“…Synthetic, semisynthetic, or natural polymers are used to prepare polymeric nanoparticles that enhance the circulation half-life, reduce the phagocytic uptake, and inactivation of drug, by which improves delivery and targeting of drugs. 14 Quality by Design (QbD) is initiated by the FDA for pharmaceutical product development (FDA guidance of industry, 2006). It is a design effort to deliberate product conceptualization for commercialization.…”

Section: Introductionmentioning

confidence: 99%

A Systematic Approach to Vildagliptin-Eudragit RL 100 Coated Nanoparticles by Combined Techniques of Solvent Evaporation and Nano-precipitation Using Quality by Design Concept

Ammanage,

Mastiholimath

2023

Int J. Pharm. Investigation

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Background: Diabetes is an endocrine disorder characterized by an abnormal increase in blood sugar level. Vildagliptin is a Dipeptidyl Peptidase-4 (DPP-4) inhibitor used in the treatment of type 2 diabetes mellitus. Purpose: The present work deals with the Quality by Design (QbD) approach based formulation and optimization of Vildagliptin-Eudragit RL 100 coated nanoparticles (VLD-EudNPs). Materials and Methods: VLD-Eud NPs were developed by combined technique of solvent evaporation and nano-precipitation. Optimization was done by 3 2 factorial designs. Prepared nanoformulations were characterized for percentage yield and morphology. Further in vitro drug release and kinetics were studied. The accelerated stability study of the optimized formulation was carried out for 3 months. Results: VLD-EudNPs ranged from 58.5±2.02 nm to 425.4±4.71 nm with a PDI of 0.27±0.036 to 0.52±0.086. Entrapment efficiency (% EE) of nanoformulations F1 to F9 ranged between 32.29±1.16 to 75.26±1.63%. The particles were found to be cylindrical-shaped, with a percentage yield of 54.7±3.45 to 84.4±1.51%. During the in vitro drug release study, at acidic pH, <5% drug release, while delayed release at basic pH, at the end of 24 hr, all formulations have released >68% of the drug following zero order kinetics. The optimized formulation has proven its stability during stability study. Conclusion: The present work concludes that prepared and optimized VLD-Eud NPs could be a better approach for sustained delivery of Vildagliptin for the management of diabetes mellitus as compared to traditional drug delivery.

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“…However, there is only one paper in this area as far as LINA is concerned in physical mixtures with two polymers, chitosan and gelatin. The optimal formulations were tested for stability at accelerated conditions (40 • C/75% RH) over a period of 1 month and finally examined by Fourier transform infrared (FT-IR) and differential scanning calorimetry (DSC) methods [13].…”

Section: Introductionmentioning

confidence: 99%

DSC, FT-IR and NIR with Chemometric Assessment Using PCA and HCA for Estimation of the Chemical Stability of Oral Antidiabetic Drug Linagliptin in the Presence of Pharmaceutical Excipients

et al. 2022

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Pharmaceutical excipients should not interact with active substances, however, in practice, they sometimes do it, affecting the efficacy, stability and safety of drugs. Thus, interactions between active substances and excipients are not desirable. For this reason, two component mixtures of oral antidiabetic drug linagliptin (LINA) with four excipients of different reactivity, i.e., lactose (LAC), mannitol (MAN), magnesium stearate (MGS) and polyvinylpyrrolidone (PVP), were prepared in a solid state. A high temperature and a high humidity of 60 °C and 70% RH, respectively, were applied as stressors in order to accelerate the potential interactions between LINA and excipients. Differential scanning calorimetry (DSC) as well as Fourier transform infrared (FT-IR) and near infrared (NIR) spectroscopy were used to estimate the changes due to potential interactions. In addition, chemometric computation of the data with principal component analysis (PCA) and hierarchical cluster analysis (HCA) was applied to adequately interpret the findings. Of the excipients used in the present experiment, all of them were not inert in relation to LINA. Some of the interactions were shown without any stressing, whereas others were observed under high-temperature/high-humidity conditions. Thus, it could be concluded that selection of appropriate excipients for LINA is very important question to minimize its degradation, especially when new types of formulations with LINA are being developed and manufactured.

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Formulation and Evaluation of Floating Polymeric Nanoparticles of Linagliptin in Capsules

Abstract: Materials Linagliptin was procured from Dr. Reddy's laboratories Ltd. Chitosan, Gelatin, sodium tri poly phosphate (STPP), glutaraldehyde, sodium bicarbonate, acetone, were procured from SD fine chemicals limited. Ethyl cellulose and HPMC E15M were procured from Yarrow Chem. Products.

Cited by 3 publications

References 3 publications

Development of Linagliptin Ultra Fine Solid Supersaturated Bio-SNEDDS Using Triangular Mixture Design for Enhancement of Oral Bioavailability: Impact of P-gp Inhibition

Development of Linagliptin Ultra Fine Solid Supersaturated Bio-SNEDDS Using Triangular Mixture Design for Enhancement of Oral Bioavailability: Impact of P-gp Inhibition

A Systematic Approach to Vildagliptin-Eudragit RL 100 Coated Nanoparticles by Combined Techniques of Solvent Evaporation and Nano-precipitation Using Quality by Design Concept

DSC, FT-IR and NIR with Chemometric Assessment Using PCA and HCA for Estimation of the Chemical Stability of Oral Antidiabetic Drug Linagliptin in the Presence of Pharmaceutical Excipients

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