Nanotechnology has shown great attention recently and become applicable in many industries. Quite recently, considerable attention has been paid to nanofillers due to their potential for excellent improved properties, such as barrier properties, high stiffness at low loadings, mechanical strength, antimicrobial, antioxidant activity, and physical, chemical, optical, and thermal stability, which increase its usage in several industries we will focus on the use the nanofillers materials in pharmaceutical applications. As the filler added to the nanoparticle may serve as an active ingredient, many nanofillers are used in several pharmaceutical applications. Nanofillers can be used in drug encapsulation to sustain and control the release of the drug, increasing the bioavailability and effect. Different nanofillers, like nanofillers that contain silver and zinc, have antimicrobial and antioxidant activity in addition to their stability. So, they could be used in drug packaging or formulated as antibacterial, antifungal, or antivirus drugs according to the filler type and the nanoparticle size, which overcome antibiotic misuse and solve the antibiotic resistance problem. Different types of nanofillers have an influential role in the wound healing process due to antimicrobial and antioxidant effect, angiogenesis modulation and their mechanical properties, and the applicability to the addition of other drugs, vitamins, or hormones. Some nanofillers have an immunomodulation role, using them as adjuvant systems for different vaccines. Nanofillers may be included in pharmaceutical preparation because they diagnose and treat acute diseases such as cancer and diabetes mellitus. Nanofillers are used during different phases in the drug industry process to help limit and eliminate pharmaceutical contaminants. Nanofillers are scaffolded for bone, skin, cardiac, and vascular regeneration. Nanofillers increase the effectiveness of many cosmetics such as dressing, creams, pads, face masks with high filtration, and cosmetic reconstruction for breast cancer. Nanofillers are used in Gene and Enzyme delivery systems, so they must be biocompatible and biodegradable. This chapter aims to illustrate the properties of nanofillers and their applications in the pharmaceutical industry and drug design.