Nanoparticles of PLGA (polylactide glycolic acid) were prepared using biodegradable poly (D, L-lactide-co-glycolide)—75？:？25, by emulsification method using PVA (Mol. Wt. 9000) or didodecyl dimethyl ammonium bromide (DMAB) as surfactant. Nanoparticles were morphologically characterized using scanning electron microscope (SEM) and particle size analyzer. The distribution of size of PLGA nanoparticles was in the range of 48–211？nm. Berberine, a yellow isoquinoline alkaloid that is used as traditional anticancer drug, was loaded on to PLGA nanoparticles by single emulsion as well as multiple emulsion solvent evaporation techniques. Particle size analysis showed an increase in berberine loaded PLGA NP size to 180–310？nm when PVA was used as a stabilizer. Whereas use of DMAB as a stabilizer led to precipitation. In vitro drug release analysis revealed that acidic pH of 5.5 was more suitable for release of berberine than pH？7.4. 1. Introduction Nanometals as well as organic nanoparticles (NP) as drug delivery devices is rapidly expanding area in drug delivery sciences. Organic polymer like polylactide glycolic acid (PLGA) has been used earlier as drug carrier because it is biocompatible as well as biodegradable [1, 2]. However, nowaday’s approaches are to use nano-sized PLGA as drug delivery vehicle. Tremendous opportunities exist for using nanoparticles as controlled drug delivery systems especially for cancer therapy so as to expose the patients with reduced doses [3–5]. Berberine, a naturally occurring isoquinoline alkaloid, is present in the roots, rhizome, and stem bark of a number of medicinal plants. Berberine has tremendous potential to cure many physiological disorders; hence, it has been used in the Ayurvedic [6], Unani, and Chinese as well as Homeopathic medicine. Berberine has been shown to inhibit activator protein 1, a key transcription factor in inflammation and carcinogenesis, in human cell lines [7] and has been shown to possess antitumor properties and effectively inhibit cyclooxygenase-2 transcriptional activity in human colon cancer cells [8, 9]. Berberine is known to inhibit DNA topoisomerase II [10]. Moreover, the antitumor properties of berberine are now recognized by researchers and clinical oncologists. The effects of berberine on human malignant brain tumor, esophageal cancer, and human leukemic and human colon cancer cell lines have been tested and significant killing effects have been achieved [1, 2, 11]. After looking into all these properties of Berberine, it was decided to try to encapsulate it in NP of PLGA for facilitated drug
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