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In the present study, the larvicidal efficacy of the extracts of the weeds Lantana camara Linn (L. camara) and Ocimum gratissimum Linn (O. gratissimum) was evaluated against the larvae of the malaria vectors A. aegypti, An. subpictus, and C. quinquefasciatus. The ethanol, n-hexane and diethyl ether crude leaf extracts were evaluated in a preliminary screening for larvicidal activity at 20,40,80,160,320 and 640 mg/l concentrations. 20 larvae of each species were introduced in different sterile Petri dishes in aqueous media under a controlled environment to assess biological activity. The larvicidal activity of both extracts was evaluated at 6 and 12-h post-exposure time points by observing the movement of each larva. The obtained data were subjected to probit analysis to determine the lethal concentrations that kill 50% and 90% (LC50 and LC90) of the treated larvae. The results revealed a noticeable larvicidal activity following 12 h of exposure. The extract of L. camara leaves exhibited an LC50 range between 18.66 and 51.35 mg/l and an LC90 range between 87.78 and 312.21 mg/l. Moreover, for the extract of O. gratissimum leaves, the LC50 range was 52.26 to 59.09 mg/l and the LC90 range was 260.22 to 348.23 mg/l. Taken together, the results indicate that the extracts of L. camara and O. gratissimum leaves may be useful as effective, economical, and eco-friendly larvicidal agents. However, additional studies are needed to explore the bioactive components of the weeds that exhibit larvicidal activity along with their mode of action. [ABSTRACT FROM AUTHOR]

The current review emphasizes on the herbal bioenhancers which themselves do not possess inherent pharmacological activity of their own but when co-administered with Active Pharmaceutical Ingredients (API), enhances their bioavailability and efficacy. Herbal bioenhancers play a crucial role in enhancing the bioavailability and bioefficacy of different classes of drugs, such as antihypertensives, anticancer, antiviral, antitubercular and antifungal drugs at low doses. This paper highlights various natural compounds that can be utilized as an efficient bioenhancer. Several herbal compounds including piperine, quercetin, genistein, naringin, sinomenine, curcumin, and glycyrrhizin have demonstrated capability to improve the pharmacokinetic parameters of several potent API. This article also focuses on various United States patents on herbal bioenhancers, which has proved to be beneficial in improving oral absorption of nutraceuticals like vitamins, minerals, amino acids and certain herbal compounds. The present paper also describes proposed mechanism of action, which mainly includes absorption process, drug metabolism, and action on drug target. The herbal bioenhancers are easily available, safe, free from side effects, minimizes drug toxicity, shortens the duration of treatment, lowers the drug resistance problems and minimizes the cost of treatment. Inspite of the fact that herbal bioenhancers provide an innovative concept for enhancing the bioavailability of several potent drugs, there are numerous bioenhancers of herbal origin that are yet to be explored in several vital areas. These bioenhancers must also be implied to enhance the bioavailability and bioefficacy through routes other than the oral route of drug delivery. There is a vast array of unexploited plants which can be investigated for their drug bioenhancing potency. The toxicity profiles of these herbal bioenhancers must not be overlooked. Researches must be carried out to solve these issues and to deliver a safe and effective dose of drugs to attain desired pharmacological response. [ABSTRACT FROM AUTHOR]

Abstract: Several methods and techniques are potentially useful for the preparation of microparticles in the field of controlled drug delivery. The type and the size of the microparticles, the entrapment, release characteristics and stability of drug in microparticles in the formulations are dependent on the method used. One of the most common methods of preparing microparticles is the single emulsion technique. Poorly soluble, lipophilic drugs are successfully retained within the microparticles prepared by this method. However, the encapsulation of highly water soluble compounds including protein and peptides presents formidable challenges to the researchers. The successful encapsulation of such compounds requires high drug loading in the microparticles, prevention of protein and peptide degradation by the encapsulation method involved and predictable release, both rate and extent, of the drug compound from the microparticles. The above mentioned problems can be overcome by using the double emulsion technique, alternatively called as multiple emulsion technique. Aiming to achieve this various techniques have been examined to prepare stable formulations utilizing w/o/w, s/o/w, w/o/o, and s/o/o type double emulsion methods. This article reviews the current state of the art in double emulsion based technologies for the preparation of microparticles including the investigation of various classes of substances that are pharmaceutically and biopharmaceutically active. [Copyright &y& Elsevier]

Abstract: Chitosan, a natural cationic polysaccharide, is prepared industrially by the hydrolysis of the aminoacetyl groups of chitin, a naturally available marine polymer. Chitosan is a non-toxic, biocompatible and biodegradable polymer and has attracted considerable interest in a wide range of biomedical and pharmaceutical applications including drug delivery, cosmetics, and tissue engineering. The primary hydroxyl and amine groups located on the backbone of chitosan are responsible for the reactivity of the polymer and also act as sites for chemical modification. However, chitosan has certain limitations for use in controlled drug delivery and tissue engineering. These limitations can be overcome by chemical modification. Thus, modified chitosan hydrogels have gained importance in current research on drug delivery and tissue engineering systems. This paper reviews the general properties of chitosan, various methods of modification, and applications of modified chitosan hydrogels. [Copyright &y& Elsevier]

Over the past several years, great advances have been made on development of novel drug delivery systems (NDDS) for plant actives and extracts. The variety of novel herbal formulations like polymeric nanoparticles, nanocapsules, liposomes, phytosomes, nanoemulsions, microsphere, transferosomes, and ethosomes has been reported using bioactive and plant extracts. The novel formulations are reported to have remarkable advantages over conventional formulations of plant actives and extracts which include enhancement of solubility, bioavailability, protection from toxicity, enhancement of pharmacological activity, enhancement of stability, improved tissue macrophages distribution, sustained delivery, and protection from physical and chemical degradation. The present review highlights the current status of the development of novel herbal formulations and summarizes their method of preparation, type of active ingredients, size, entrapment efficiency, route of administration, biological activity and applications of novel formulations. [Copyright &y& Elsevier]

Development of natural mosquito repellants is essential considering their safety profile unlike synthetic insecticides. Herein, novel liquid vaporizable preparations of the essential oils obtained from the leaves of weeds Lantana camara Linn (L. Camara) family Verbenaceae, and Ocimum gratissimum Linn (O. gratissimum) family Lamiaceae were developed for the evaluation of mosquitocidal and larvicidal activities against malaria vectors, Anopheles subpictus, Aedes aegypti and Culex quinquefasciatus. While mosquitocidal effect was evaluated as knockdown of mosquitoes in modified glass chamber for an exposure period of 1 h, larvicidal activity was assessed as inhibition of larval motility in petri dish at intervals of 6-, 12- and 24-hr. Combination of essential oils of L. Camara and O. gratissimum leaves prepared in ethyl alcohol at 1:5 ratio exhibited maximum synergistic mosquitocidal effect against all three test species (94–97%). This effect was comparable with that of standard 1:1 combination ratio of essential oils of Cymbopogon nardus (L.) Rendle and Eucalyptus globulus Labill. Furthermore, statistical analysis using probit regression model for determination of LC50 and LC90 revealed excellent larvicidal effect of essential oil of O. gratissimum leaves at 24-hr time-point (LC50 = 40.08 ± 1.60 ppm and LC90 = 78.035 ± 1.90 ppm). Our data suggest the lethal effects of essential oils of L. camara and O. gratissimum leaves on Anopheles subpictus, Aedes aegypti and Culex quinquefasciatus. Therefore, essential oil preparations of these weeds can be used as natural, harmless and inexpensive mosquito repellents. • Essential oils of L. Camara and O. gratissimum leaves were evaluated for larvicidal and mosquitocidal activities. • O. gratissimum showed higher larvicidal activity than that of L. Camara. • Larvicidal effect of L. camara and O. gratissimum were LC50 = 45.32 ppm and LC50 = 40.08 ppm, respectively. • Exposure of rats to both essential oils did not exhibit any sign of toxicity. • The proposed preparations may be an effective, safe and cheap alternative to the synthetic mosquito repellents. [ABSTRACT FROM AUTHOR]

Highlights • Already available conventional formulations limit the use of existing conventional formulations. • Nanocarrier based formulations are a promising prospect to overcome the existing limitations. • Present review underlines the novel strategies towards psoriasis treatment. Abstract Psoriasis is a consistently recurring, inflammatory, autoimmune disorder of the skin, affecting about 2–5% of the world population. Abundant therapeutic agents are accessible for the treatment of psoriasis. Nevertheless, none of them are entirely secure and effective to treat the disease without compromising patient compliance. Furthermore, already existing drugs are supposed to restrain the ailment and alleviate the sign and symptoms with no complete cure. However, they focus on restraining the disease and alleviating the symptoms without providing an absolute cure. Therefore there remains a vital challenge, to explore a new drug moiety or delivery system which could safely and effectively manage psoriasis without compromising patient compliance. Furthermore, conventional formulations offer reduced benefit/risk ratio of anti-psoriatic drugs, which limits the use of existing conventional formulations. Novel formulations based on nanocarriers are a promising prospect to overcome the limitation of conventional formulations by offering a reduction in dose, dosing frequency, dose-dependent, side effects with enhanced efficacy. Presently nano-formulations have gained widespread application for effective and safe treatment of psoriasis. The present review primarily focuses on conventional therapeutic strategy and recent advances in lipid-based, polymer-based and metallic nano-formulations of a variety of anti-psoriatic drugs. The practicability of various nanocarrier systems including liposomes, nanostructured lipid carriers, ethosomes, solid lipid nanoparticles, nanocapsules, micelles, dendrimers, gold nanoparticles and silver nanoparticles have been discussed in detail. The review also traces related patents to exemplify the role of various nanoparticles in psoriasis treatment. In a nutshell, nano-formulations remain established as a promising modality for treating psoriasis treatment as they propose better penetration, targeted delivery, enhanced safety, and efficacy. [ABSTRACT FROM AUTHOR]

Utilizing the diverse features of biocompatible polymers to target drugs into the tumor/s has been a research hotspot since last decade. Such polymeric conjugates of anti-cancer drugs have proven their potential in providing sustained release of drugs with reduced systemic toxicity and improved tumor retention. Polymers like polyethylene glycol (PEG), N-(2-Hydroxypropyl) methacrylamide (HPMA), Polylactic-co-glycolic acid (PLGA), Polyamidoamine (PAMAM), and others remain exploited for their specific as well as shared characteristics in the rational delivery of anti-cancer agents. Variable nano size, attachment with tumor-specific proteins, responsiveness to stimuli and ability to deliver a wide range of molecules like drugs, antibodies and peptides are some of the achievements of polymeric nano-conjugates so far. Many such conjugates have shown potential clinically which has attracted the researchers and promoted further advancements of the technique. Apart from achievements the polymeric conjugates suffer from shortcomings like poor drug loading and chances of potential chronic-systemic toxicities. The review highlights key findings of research in recent time and advancements taking place in the field of polymeric conjugates of anti-cancer drugs along with the limitations. We have also emphasized on newer and relatively less explored applications of tumor-targeted polymeric conjugates which can add new dimensions to this technique. [ABSTRACT FROM AUTHOR]

Although paclitaxel is a front-line chemotherapeutic agent for the treatment of metastatic breast cancer, its intravenous therapy produces deleterious adverse effects. In an attempt to address the issue, the present study aimed to develop a paclitaxel loaded thermosensitive/thermoresponsive hydrogel (PTXNp-TGel) for loco-regional administration to breast tumors to provide dose-dense chemotherapy. Poloxamer and xanthan gum were used to prepare TGel by the cold method. In vitro and in vivo performance of PTXNp-TGel was compared with TGel, pure drug loaded TGel (PTX-TGel) and marketed formulation, Taxol®. The formulated PTXNp-TGel showed acceptable gelation temperature and time (37 °C and 57 s), lower viscosity at room temperature and higher viscosity at body temperature to support sol-gel transition with increasing temperature, and sustained drug release up to 21 days. Additionally, PTXNp-TGel showed negligible hemolytic toxicity as compared to PTX-TGel and Taxol®. Intratumoral administration of PTXNp-TGel produced significantly higher antitumor activity as indicated by lowest relative tumor volume (1.50) and relative antitumor proliferation rate (27.71 %) in comparison with PTX-TGel, Taxol®, and PTXNp (p < 0.05). Finally, insignificant body weight loss during the experimental period, lack of hematotoxicity, nephrotoxicity, and hepatotoxicity imply improved therapeutic performance of the locally administrated dose-dense therapy of PTXNp-TGel as compared to Taxol®. • Paclitaxel loaded thermoresponsive hydrogel (PTXNp-TGel) provided dose dense chemotherapy in breast cancer model. • Xanthan gum provided mucoadhesive character to PTXNp-TGel and helped in retention of gel at the tumor site. • Loco regional administration of PTXNp-TGel exhibited remarkable antitumor activity without any significant side effects. • Same delivery system can be used for other cytotoxic agents to improve their therapeutic efficacy. [ABSTRACT FROM AUTHOR]

The effect of Ca 2+ ion cross-linker on acryalamide grafted carboxymethyl xanthan gum (CMXG-g-PAAm) on the drug release was investigated. Previously, CMXG was synthesized from XG and further grafted to CMXG-g-PAAm to retard the drug release. Once the CaCl 2 solution is added to CMXG-g-PAAm, Ca 2+ considerably affected the drug release mechanism mainly by diffusion and erosion. In order to validate the grafted polymer, tablets were prepared using wet granulation and dry granulation methods It has been noticed that the tablets prepared by wet granulation successfully controls the release of the drug over an extended period of time. Moreover, the release profile was aligned to Korsmeyer–Peppas equation and exhibited the drug transport mechanism via diffusion and erosion. [ABSTRACT FROM AUTHOR]

In the present work, an unreported graft copolymer of carboxymethyl xanthan gum and acrylamide has been synthesised by free radical polymerisation in a nitrogen atmosphere using ammonium persulphate as an initiator. The optimum reaction conditions adopted for affording maximum percentage of grafting including its grafting efficiency were obtained by varying the concentration of carboxymethyl xanthan gum from 4 to 24 g dm −3 ; ammonium persulphate from 5 × 10 −4 to 30 × 10 −4 mol dm −3 ; acrylamide from 0.4 to 1.2 mol dm −3 ; reaction temperature from 55 to 75 °C and reaction time from 30 to 90 min. The synthesised graft copolymer has been characterised by 1 H NMR, FTIR spectroscopy, X-ray diffraction measurement, thermal analysis, viscosity measurement and scanning electron microscopy. However, grafting of acrylamide onto carboxymethyl xanthan gum backbone enhanced its thermal stability. This graft copolymer might be well exploited globally as a potential carrier for drug delivery system. [ABSTRACT FROM AUTHOR]

Diabetes associated oxidative stress and impaired cholinergic neurotransmission causes cognitive deficits. Although phloridzin shows antioxidant- and insulin sensitizing-activities, its ameliorative potential in diabetes-induced memory dysfunction remains unexplored. In the present study, type 2 diabetes (T2D) was induced by streptozotocin (35 mg/kg, intraperitoneal) in rats on ad libitum high-fat diet. Diabetic animals were treated orally with phloridzin (10 and 20 mg/kg) for four weeks. Memory functions were evaluated by passive avoidance test (PAT) and novel object recognition (NOR) test. Brains of rats were subjected to biochemical analysis of glutathione (GSH), brain-derived neurotrophic factor (BDNF), malonaldehyde (MDA) and acetylcholinesterase (AChE). Role of cholinergic system in the effects of phloridzin was evaluated by scopolamine pre-treatment in behavioral studies. While diabetic rats showed a significant decrease in step through latency in PAT, and exploration time and discrimination index in NOR test; a substantial increase in all parameters was observed following phloridzin treatment. Phloridzin reversed abnormal levels of GSH, BDNF, MDA and AChE in the brain of diabetic animals. Moreover, in silico molecular docking study revealed that phloridzin acts as a potent agonist at M1 receptor as compared to acetylcholine. Viewed collectively, reversal of T2D-induced memory impairment by phloridzin might be attributed to upregulation of neurotrophic factors, reduced oxidative stress and increased cholinergic signaling in the brain. Therefore, phloridzin may be a promising molecule in the management of cognitive impairment comorbid with T2D. • Cognitive deficit in diabetes is linked with oxidative stress, impaired neuroprotection and cholinergic neurotransmission. • Phloridzin is a flavonoid with promising antioxidant and insulin sensitizing actions in type 2 diabetes. • Four weeks treatments with phloridzin significantly reversed cognitive deficit in diabetic rats. • Phloridzin enhanced cholinergic neurotransmission, antioxidant defense and neurotrophic factor in the brain of diabetic rats. • Phloridzin may have therapeutic potential in the management of cognitive impairment associated with diabetes. [ABSTRACT FROM AUTHOR]

Anemia is the most common hematological abnormality of chemotherapy, which is responsible for poor clinical outcomes. To overcome this complication, the present study was aimed for developing a Eudragit/polylactic-co-glycolic acid (PLGA) based nanoparticulate system for a model drug paclitaxel (PTX). The study was planned using a simplex lattice mixture design. PTX nanoparticles (PTXNp) were evaluated in vitro for physicochemical properties, hemolytic effects and cytotoxic effects. Further, the nanoparticles were subjected to in vivo screening using rats for hemocompatibility, pharmacokinetic profile, and biodistribution to the vital organs. The PTXNps were 65.77–214.73 nm in size, showed more than 60% sustained drug release in 360 h and caused less than 8% hemolysis. The parameters like red blood cell count, activated partial thromboplastin time (aPTT), prothrombin time (PT) and C3 complement were similar to the negative control. Cytotoxicity results suggested that all the PTXNp demonstrated drug concentration-dependent cytotoxicity. The in vivo pharmacokinetic study concluded that PTXNp formulations had significantly higher blood AUC (93.194.55–163,071.15 h*ng/mL), longer half-lives (5.80–6.35 h) and extended mean residence times (6.05–8.54 h) in comparison to PTX solution (p < 0.05). Overall, the study provides a nanoparticulate drug delivery system to deliver PTX safely and effectively along with reducing the associated hematological adverse effects. [Display omitted] • A simplex lattice mixture design of experiment was used to study the influence of formulation polymers (ERSPO, ERLPO and PLGA) and their respective concentrations on particle size, hemolysis and drug release. • Lastly, the three optimized nanoparticles were evaluated in vitro and in vivo specifically for their pharmacokinetic profile, biodistribution studies, and hemocompatibility studies. • The optimized PTX nanoparticles demonstrated significant hemocompatibility as compared to pure drug solution. • The mean AUC and terminal half-life of PTX upon IV administration of PTXNp was significantly higher than from pure PTX solution. [ABSTRACT FROM AUTHOR]

Objectives: To investigate primary angioplasty (PA) for high-risk acute myocardial infarction (AMI) at hospitals with no cardiac surgery on-site (No SOS), we hypothesized that a nonrandomized registry of such patients treated with PA would show clinical outcomes similar to those of a group randomized to transfer for PA, and that reperfusion would occur faster.Background: Primary angioplasty provides outcomes superior to fibrinolytic therapy in AMI, but its use in community hospitals with No SOS has been limited.Methods: Fibrinolytic-eligible patients with high-risk AMI prospectively consented if they had one or more high-risk characteristic. Nineteen hospitals with No SOS prospectively enrolled 500 patients for PA on-site. Seventy-one similar Air Primary Angioplasty in Myocardial Infarction trial patients were randomized to transfer for PA.Results: Primary angioplasty was performed in 88% of patients. Patients transferred for PA had a longer mean time to treatment (187 vs. 120 min; p < 0.0001). Thrombolysis In Myocardial Infarction (TIMI) flow grade 3 was achieved in 96% for on-site PA, 86% in the transfer group (p = 0.004). The combined primary end point of 30-day mortality, re-infarction, and disabling stroke occurred in 27 (5%) on-site PA patients and 6 (8.5%) transfer patients (p = 0.27). Unadjusted one-year mortality was improved in on-site PA patients compared with those transferred (6% vs. 13%, p = 0.043), but after adjustment for differences in baseline variables, this difference was not significant.Conclusions: On-site PA and transfer groups had similar 30-day outcomes and more rapid reperfusion for on-site PA. Primary angioplasty in high-risk AMI patients at hospitals with No SOS is safe, effective, and faster than PA after transfer to a surgical facility. [Copyright &y& Elsevier]

Herbal antioxidant like curcumin holds great potential to treat neurodegenerative disease like Alzheimer's disease. However, its therapeutic potency is obstructed due to rapid metabolism, poor solubility, GI susceptibility, enzymatic degradation and lower bioavailability. Thus, the present work aimed to design and optimize curcumin-loaded NLC (CNL) with higher drug entrapment, prolonged release and better stability. CNL was prepared by modified melt emulsification method followed by ultrasonication. The formulation was optimized by 3 factor 3 level Box-Behnken design using solid: liquid lipid, surfactant concentration and ultrasonication time as independent variable while particle size, entrapment efficiency and % drug release as dependant variable. The design suggested 3.092 solid:liquid lipid, 2.131% surfactant and 4.757 min ultrasonication fit best to get the optimized formulation. The size of the optimized CNL was noted 124.37 ± 55.81 nm, which is in the acceptable range for brain delivery. SEM results also comply with this size range (near 150 nm) and demonstrated almost spherical and uniform particles with porous and uneven surface structures. PDI, zeta potential, entrapment efficiency and % drug release were observed as 0.201 ± 0.00, − 17.2 ± 2.35 mV, 93.62 ± 0.68% and 92.73 ± 0.06%, respectively. The NLC demonstrated initial burst release with subsequent prolonged release of drug for 48 h. Weibull kinetic equation with 0.9958 R2, minimum AIC and maximum MSC value was found best fit to explain the release behavior. The β exponent and diffusional coefficient (n) indicated combined release mechanism with Fickian diffusion as drug release mechanism. Formulation was also found stable at different storage condition. [Display omitted] • Imperfect lattice structure of NLC greatly enhances drug entrapment efficiency. • Drug loaded NLC was prepared by melt-emulsification ultrasonication method. • Effect of solid:liquid lipid, surfactant concentration on formulation was optimized. • Initial burst release with subsequent sustained release of 92.73% drug. • Weibull kinetic exponent showed combined release mechanism with Fickian diffusion. [ABSTRACT FROM AUTHOR]

• Poor aqueous solubility of bortezomib: major drawback in formulation development. • Bortezomib encapsulation in PEGylated PAMAM dendrimers. • Cytotoxicity assay against A549 and MCF-7 cancer cells. • In vivo pharmacokinetic studies co-relating the in vitro results. Poor aqueous solubility of anticancer drug bortezomib (BTZ) still remains a major challenge in the development of a successful formulation. The dendrimeric platform can provide a better opportunity to deliver BTZ with improved solubility. BTZ encapsulated in PEGylated PAMAM dendrimers (BTZ-PEG-PAMAM) was characterized and evaluated comparatively with encapsulated and conjugated dendritic formulations. The particle size of BTZ-PEG-PAMAM was 188.6 ± 4.17 nm, with entrapment efficiency of 78.61 ± 2.91% and drug loading of 39.30 ± 1.98%. The aqueous solubility of BTZ in PAMAM-PEG conjugate was enhanced by 68.11 folds in comparison to pure drug. In vitro drug release profile was found to be sustained up to 72 h. A comparative colorimetric MTT assay against A549 and MCF-7 cancer cells resulted in maximum efficacy from BTZ-PEG-PAMAM with IC 50 value 333.14 ± 15.42 and 152.60 ± 24.56 nM, respectively. Significantly higher cellular internalization was observed in FITC tagged BTZ-PEG-PAMAM. In vivo pharmacokinetic study performed on Sprague Dawley rats resulted in 8.63 folds increase in bioavailability for BTZ-PEG-PAMAM than pure drug. Pharmacokinetic parameters of BTZ-PEG-PAMAM were better and improved over BTZ and other dendritic formulations. In conclusion, the prepared formulation of BTZ-PEG-PAMAM has given significant outcome and this strategy may be further explored for better delivery of BTZ in future. [ABSTRACT FROM AUTHOR]

• Synthesis and evaluation of conjugates; HPMA-Biotin, HPMA-PLA, HPMA-PLA-Biotin. • Effect of biotin as a targeting ligand on breast cancer cells. • Two folds reduction in IC 50 values of HPLA-BT PNPs than pure BTZ. • Cellular uptake interactions of PNPs in breast cancer cells. • In vivo data (bioavailability, t1/2, v d) supported in vitro results. Bortezomib (BTZ) is a proteasome inhibitor as approved by US FDA for the treatment of multiple myeloma. It exhibits significant anti-cancer properties, against solid tumors; but lacks aqueous solubility, chemical stability which hinders its successful formulation development. The present study is an attempt to deliver BTZ using N-(2-hydroxypropyl) methacrylamide (HPMA) based copolymeric conjugates and biotinylated PNPs in an effective manner. Study describes a systematic synthetic pathway to synthesize functional polymeric conjugates such as HPMA-Biotin (HP-BT) HPMA-Polylactic acid (HPLA) and HPMA-PLA-Biotin (HPLA-BT) followed by exhaustive characterization both spectroscopically and microscopically. Our strategy yielded polymeric nanoparticles (PNPs) of narrow size range of 199.7 ± 1.32 nm. Release studies were performed at pH 7.4 and 5.6. PNPs were 2-folds less hemolytic (p < 0.0001) than pure drug. BTZ loaded PNPs of HPLA-BT demonstrated significant anti-cancer activity against MCF-7 cells. IC 50 value of these PNPs was 56.06 ± 0.12 nM, which was approximately two folds less than BTZ (p < 0.0001). Cellular uptake study confirmed that higher uptake of formulations might be an outcome of biotin surface tethering characteristics that enhanced selectivity and targeting of formulations efficiently. In vivo pharmacokinetics evidenced increased bioavailability (AUC 0 t-∞) of DL-HPLA-BT PNPs (drug loaded) than BTZ with an improved half-life. Overall the developed PNPs led to the improved and effective BTZ delivery. [ABSTRACT FROM AUTHOR]