Dental caries is the world's biggest dental problem with an incidence of 95%, causing tooth demineralization and complications including pulp perforation and premature tooth loss. A non-toxic biomaterial is required for increasing dentine regeneration in reversible dental caries. Proanthocyanidin (PA) is grape seed-derived flavonoid as antibacterial, anti-inflammatory, and antioxidant. However, PA provides low bioavailability so that it can be combined with polyamidoamine-calcium phosphate (PAMAM-CP) nanoparticles as drug delivery system. The investigation of PA and PAMAM-CP nanoparticles paste-based as innovation biomaterial for dental pulp capping may potential to induce dentine regeneration. The aim of this narrative review is to describe the combination of PA and PAMAM-CP nanoparticles as dental pulp capping biomaterial for dentin regeneration in dental caries. PA is able to express runt related transcription factor (Runx2), bone morphogenic protein-2 (BMP2), osteocalcin (OCN), and dentine sialophospoprotein (DSPP) which increase biomineralization and odontogenic differentiation. PAMAM is a macromolecule that provides attachment to dentine and induces remineralization. CP nanoparticles are calcium phosphate-based drug carriers that facilitate dentinal tubules penetration. PA loaded PAMAM-CP nanoparticles would be encapsulated releasing PA. PA suppresses Nuclear Factor-kB signaling pathway activation and decrease tumor necrosis factor-α so that inhibit dentinal matrix degradation. PA increases Runx2 and DSPP expression that manifest in dental pulp stem cells differentiation into odontoblasts. Combination of PA and PAMAM-CP nanoparticles may potential and beneficial as pulp capping biomaterial for dentin regeneration in dental caries.