Zero order controlled release delivery of cholecalciferol from injectable biodegradable microsphere: In-vitro characterization and in-vivo pharmacokinetic studies

Vora, Lalitkumar K.; Sita, V G; Vavia, Pradeep R.

doi:10.1016/j.ejps.2017.06.027

Cited by 34 publications

(14 citation statements)

References 29 publications

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“…Biodegradable polymers of the aliphatic polyester family are PLGA and PLA, which have already been frequently applied in tissue engineering and drug delivery. PLGA, a copolymer of PLA and PGA, is the best defined biodegradable polymer in the controlled release of encapsulated drug and, is widely used for sustained drug release at desirable doses by implantation without surgical methods [170,171]. Additionally, the overall physical properties of the polymer-drug matrix can be tuned by controlling the relevant factors such as the ratio of lactide to glycolide, drug concentration and, polymer molecular weight to achieve a desired dosage and release period varying upon the drug type [170].…”

Section: Plga/pla Mnsmentioning

confidence: 99%

Microneedle array systems for long-acting drug delivery

Vora

Moffatt

Tekko

et al. 2021

European Journal of Pharmaceutics and Biopharmaceutics

178

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Section: Plga/pla Mnsmentioning

confidence: 99%

Microneedle array systems for long-acting drug delivery

Vora

Moffatt

Tekko

et al. 2021

European Journal of Pharmaceutics and Biopharmaceutics

178

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“…VD 3 has been successfully formulated and administrated transdermally and subcutaneously by using different vehicles, including nanocarriers [37][38][39]. However, our proposed system presents a potential advantage, which is reduction of the administration frequency.…”

Section: Accepted Manuscriptmentioning

confidence: 99%

Novel bilayer dissolving microneedle arrays with concentrated PLGA nano-microparticles for targeted intradermal delivery: Proof of concept

Vora

Donnelly

Larrañeta

et al. 2017

Journal of Controlled Release

124

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Polymeric microneedle (MN) arrays continue to receive growing attention due to their ability to bypass the skin's stratum corneum barrier in a minimally-invasive fashion and achieve enhanced transdermal drug delivery and "targeted" intradermal vaccine administration. In this research work, we fabricated biodegradable bilayer MN arrays containing nano - microparticles for targeted and sustained intradermal drug delivery. For this study, model drug (vitamin D, VD)-loaded PLGA nano- and microparticles (NMP) were prepared by a single emulsion solvent evaporation method with 72.8% encapsulation of VD. The prepared NMP were directly mixed 20% w/v poly(vinyl pyrrolidone) (PVP) gel, with the mixture filled into laser engineered micromoulds by high-speed centrifugation (30min) to concentrate NMP into MN shafts. The particle size of PLGA NMP ranged from 300nm to 3.5μm and they retained their particle size after moulding of bilayer MN arrays. The relatively wide particle size distribution of PLGA NMP was shown to be important in producing a compact structure in bilayer conical, as well as pyramidal, MN, as confirmed by scanning electron microscopy. The drug release profile from PLGA NMP was tri-phasic, being sustained over 5days. The height of bilayer MN arrays was influenced by the weight ratio of NMP and 20% w/v PVP. Good mechanical and insertion profiles (into a skin simulant and excised neonatal porcine skin) were confirmed by texture analysis and optical coherence tomography, respectively. Ex vivo intradermal neonatal porcine skin penetration of VD NMP from bilayer MN was quantitatively analysed after cryostatic skin sectioning, with 74.2±9.18% of VD loading delivered intradermally. The two-stage novel processing strategy developed here provides a simple and easy method for localising particulate delivery systems into dissolving MN. Such systems may serve as promising means for controlled transdermal delivery and targeted intradermal administration.

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“…Dissolving microneedles efficiently deliver therapeutic agents through the dissolution of their biocompatible polymer matrices after penetration into the skin (Vora, Donnelly, et al, ; Vora, Sita, & Vavia, ). DMNs rely on the water solubility of both the loaded drug and the polymer matrix.…”

Section: Introductionmentioning

confidence: 99%

Novel nanosuspension‐based dissolving microneedle arrays for transdermal delivery of a hydrophobic drug

Vora

Vavia

Larrañeta

et al. 2018

J of Interdiscip Nanomed

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A nanosuspension (NS) was formulated from the lipophilic molecule cholecalciferol (CL) for enhanced transdermal delivery by embedding this NS into hydrophilic polymer‐based dissolving microneedles (DMNs). First, the NS was prepared by sonoprecpitation with different molecular weights of poly (vinyl alcohol) and poly (vinyl pyrrolidone) as stabilizers and using two different solvents for particle size and zeta potential optimization. DMN arrays were then prepared by centrifugation‐assisted micromoulding and subsequently dried. Poly (vinyl alcohol) (10 kDa) produced a NS with the lowest particle size ( ~ 300 nm). These particles yielded DMN with good mechanical properties when combined with aqueous blends of high molecular weight poly (vinyl pyrrolidone) (360 kDa). The particle size remained similar before and after MN preparation, as confirmed by scanning electron microscope. The CL was in the amorphous state in the free particles as well as in the DMN and, hence, no characteristic CL peak was observed in differential scanning calorimetry or X‐ray diffraction. DMN arrays were found to be strong enough to bear a 32 N force, showed efficient skin insertion, and penetrated down to the third layer (depth ≈ 375 μm) of the validated skin model Parafilm M®. An ex vivo porcine skin permeation study using Franz diffusion cells compared the permeation of CL from CL‐NS‐loaded DMN arrays and MN‐free CL‐NS patches. It was observed that CL‐NS‐loaded DMN arrays showed significantly higher (498.19 μg ± 89.3 μg) ex vivo skin permeation compared with MN‐free CL‐NS patches (73.2 μg ± 26.5 μg) over 24 h. This is the first time a NS of a hydrophobic drug has been successfully incorporated into dissolving MN and suggest that NS‐containing DMN systems could be a promising strategy for transdermal delivery of hydrophobic drugs.

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Zero order controlled release delivery of cholecalciferol from injectable biodegradable microsphere: In-vitro characterization and in-vivo pharmacokinetic studies

Cited by 34 publications

References 29 publications

Microneedle array systems for long-acting drug delivery

Microneedle array systems for long-acting drug delivery

Novel bilayer dissolving microneedle arrays with concentrated PLGA nano-microparticles for targeted intradermal delivery: Proof of concept

Novel nanosuspension‐based dissolving microneedle arrays for transdermal delivery of a hydrophobic drug

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