Solid lipid dispersion of calcitriol with enhanced dissolution and stability

Yuan, Ting; Qin, Lingzhen; Wang, Zhouhua; Nie, Jinyuan; Guo, Zhefei; Li, G e; Wu, Chuanbin

doi:10.1016/j.ajps.2013.07.005

Cited by 11 publications

(6 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Due to this reason 4%v/v of OLMS is used in formulation. TPGS is an effective solubilizing agent and coemulsifying agent which helps to achieve more uniform size nanoparticles [27]. It is a low melting solid hence get precipitated at the end of process of SLN formulation.…”

Section: Discussionmentioning

confidence: 99%

Influence of Various Process Variables and Formulation Excipients on the Engineering of Sertaconazole Solid Lipid Nanoparticles

Baviskar¹

2016

IOSRPHR

View full text Add to dashboard Cite

Abstract:The present research work focuses on the study of influence of various ingredients, concentration of ingredients and process parameters on the formulation of Solid lipid nanoparticles (SLN). The sertaconazole loaded solid lipid nanoparticles (SERT-SLN) were prepared by simple, easily reproducible and novel modified solvent emulsification method. Lipid and surfactant solubilizing potential was determined by solubility study. To improve the properties of SLN some excipients were added like cosurfactant TPGS, organic solvent for nanodroplet structure in SLN and charge induction by stearyl amine. Further study was performed to determine the optimum concentration of components such as concentration of surfactant OLML, stearyl amine, TPGS and organic solvent. The process parameters like stirring rate and time, sonication time and cooling temperature also affect the formation of SLN. The formulations were evaluated for average particle size, polydispersity index (PDI) and zeta potential (ZP). The particle size, PDI and ZP of optimized formulation was observed to be 155.1 nm, 0.23 and 9.76 mV respectively. The TEM study confirms the nanometric size particles with particle size < 200 nm. The DSC and XRD study reveals the presence of amorphous nature of SLN. The SERT-SLN formulation was stable at refrigerator and 25 0 C. SERT-SLN showed biphasic release pattern initiated with burst and then sustained release.

show abstract

Section: Discussionmentioning

confidence: 99%

Influence of Various Process Variables and Formulation Excipients on the Engineering of Sertaconazole Solid Lipid Nanoparticles

Baviskar¹

2016

IOSRPHR

View full text Add to dashboard Cite

show abstract

“…3,11,12 Additionally, SLNs have some other advantages such as (i) enhanced bio-absorption of encapsulated drug, (ii) ability to modify the drug release behavior, (iii) improvement of tissue distribution and (iv) drug targeting via surface engineering. 13,14 Furosemide (FRS) is a high ceiling diuretic given in the management of edema linked with cardiac, renal, and hepatic failure and the treatment of hypertension. It is a BCS class IV drug because of its low solubility and low permeability, which result in reduced bioavailability.…”

Section: Introductionmentioning

confidence: 99%

In vitro–in vivo and pharmacokinetic evaluation of solid lipid nanoparticles of furosemide using Gastroplus™

et al. 2017

View full text Add to dashboard Cite

show abstract

“…These findings are in accordance to a previous report which demonstrated improved the stability of calcitriol with a lipid-based formulation. 21 Also, a polymeric formulation demonstrated good stability profile of cholecalciferol at different conditions of storage. 31…”

Section: Stability Studymentioning

confidence: 92%

“…17 Keeping these aspects into consideration, novel formulation strategies are required for the efficient delivery of cholecalciferol. 18 Various delivery options have been explored to prevent the degradation of cholecalciferol including casein micelles, 19 zein nanoparticles coated with carboxymethyl chitosan, 14 carboxymethyl chitosan-soy protein complex nanoparticles, 20 solid dispersion, 21 and microspheres. 22 In the present study a solid dispersion-based formulation was developed to improve the solubility of cholecalciferol and developed solid dispersion was subsequently encapsulated in the HPMC based delayed release capsules which offer protection of cholecalciferol from the low pH of the stomach.…”

Section: Introductionmentioning

confidence: 99%

Delayed Release HPMC Capsules for Efficient Delivery of Cholecalciferol Solid Dispersion

Rawat¹,

Khan²,

Singh³

et al. 2023

Ind. J. Pharm. Edu. Res.

View full text Add to dashboard Cite

Introduction:The deficiency of Vitamin D is associated with an increased risk of various diseases and deficiency of this Vitamin is recognized in individuals all over the world. Therefore, the intake of Vitamin D has become essential. Objectives: Cholecalciferol (Vitamin D 3 ) is a poorly soluble molecule and it is very sensitive to degradation under environmental factors such as light, temperature, and oxygen. Its stability is also affected adversely under acidic conditions. Therefore, solid dispersion-based formulation for cholecalciferol was developed and encapsulated in delayed release hydroxypropylmethyl cellulose (HPMC) capsules. Materials and Methods: Cholecalciferol solid dispersion was developed and characterized by Fourier transform-infra red spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and X-ray diffraction analysis. The effect of various concentrations of cholecalciferol formulations on the viability of Caco-2 cells was determined by using MTT assay. Dissolution profile and stability study of the developed product was also evaluated. Results: The results demonstrated improved solubility of cholecalciferol in solid dispersion-based formulation. The drug content of solid dispersions was in the order of 91±2.3% and various studies showed the amorphous form of cholecalciferol in the solid dispersion. The cell viability assay in Caco-2 cells demonstrated that the surfactant used in the solid dispersion formulation of cholecalciferol had no adverse effect on intestinal cells. Further, dissolution profile of HPMC capsule encapsulated solid dispersion showed improved dissolution of cholecalciferol. Moreover, the stability study indicated no significant changes in the cholecalciferol content in the developed formulation under storage at experimental conditions. Conclusion: The solid dispersion-based formulation of cholecalciferol exhibited improved solubility and found to be compatible with Caco-2 cells. The delayed release HPMC capsule encapsulated solid dispersion of cholecalciferol (DRHCap-SD) showed improved dissolution and acceptable stability profile and this represent a potential delivery system for oral administration of cholecalciferol.

show abstract

Solid lipid dispersion of calcitriol with enhanced dissolution and stability

Cited by 11 publications

References 29 publications

Influence of Various Process Variables and Formulation Excipients on the Engineering of Sertaconazole Solid Lipid Nanoparticles

Influence of Various Process Variables and Formulation Excipients on the Engineering of Sertaconazole Solid Lipid Nanoparticles

In vitro–in vivo and pharmacokinetic evaluation of solid lipid nanoparticles of furosemide using Gastroplus™

Delayed Release HPMC Capsules for Efficient Delivery of Cholecalciferol Solid Dispersion

Contact Info

Product

Resources

About