Development of an oral organic-inorganic hybrid nanocomposite for prolonged sustained release of nifedipine

doi:10.5246/jcps.2025.07.045

Abstract

Abstract:

Nifedipine (NF), a widely prescribed antihypertensive agent, necessitates long-term administration to maintain therapeutic efficacy. Although osmotic pump formulations, such as Bayer’s Adalat^®, are well-established for achieving zero-order drug release, their complex manufacturing requirements significantly elevate production costs. In this study, we employed mesoporous silica as a drug carrier for nifedipine and incorporated it with an organic polymer matrix to construct an organic-inorganic hybrid nanocomposite (OIN). This nanostructured system demonstrated robust sustained-release properties in both in vitro and in vivo evaluations, with the in vitro release profile exhibiting classical first-order kinetics. To further optimize the release behavior, we combined OIN with conventional tablet-forming techniques to create an oral nanocomposite system (ONS) capable of achieving near-zero-order release. Remarkably, the cumulative release profiles of ONS closely mirrored those of the commercially available Adalat^® osmotic formulation across multiple time points. Moreover, we conducted a theoretical analysis of the release mechanisms underlying both OIN and ONS systems, offering novel mechanistic insights that could inform the future design of advanced sustained-release drug delivery platforms.

Key words: Nifedipine, Organic-inorganic hybrid nanocomposite, Zero-order release, Silica, Eudragit? RSPO

Supporting:

Jia Yan, Yanqin Liang, Cuishuan Wu, Qiang Zhang. Development of an oral organic-inorganic hybrid nanocomposite for prolonged sustained release of nifedipine[J]. Journal of Chinese Pharmaceutical Sciences, 2025, 34(7): 605-621.

Figures/Tables 16

Table 1. Orthogonal experimental design based on the types and ratios of silica and sustained-release materials.

Table 2. Preparation of different OINs.

Table 3. Fitting results of in vitro drug release curves for various OINs.

Table 4. Several formulations for the production of tablets.

Table 5. Formulation design for sustained-release materials added in equal amounts based on Formula 3 in Table 4 (The names of the formulations were designated based on the names of the sustained-release materials added).

Table 6. The formulation design for Tablet A and Tablet B coated with two different coatings (Coating 1= Opadry®, Coating 2= Acryl-EZE®).

Table 7. Fitting results of in vitro drug release curves of ONS and Adalat®.

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