Enhanced solubility and permeability of exemestane solid dispersion powders for improved oral delivery

Basanth Babu Eedara,Mradul Kankane,Raju Jukanti,Vijay Kumar Nagabandi,Suresh Bandari 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.3

The aim of the present investigation was to enhance the solubility of exemestane (EXM), by solid dispersion (SD) technique using PEG 6000 as a carrier. Phase solubility studies were conducted with PEG 6000and PEG 20000 to evaluate the effect of carriers on aqueous solubility of EXM. The aqueous solubility of EXM was favoured with PEG 6000 compared to PEG 20000. SDs of EXM using polyethylene glycol 6000 (PEG 6000) as carrier were prepared in different drug to carrier ratios. Solid-state characterization indicated decrease in crystallinity of the drug. The in vitro dissolution rate of EXM was enhanced from both SDs and tablet formulations prepared using SD compared to pure EXM. The in situ permeability studies investigated using single-pass intestinal perfusion technique in rats revealed increase in effective intestinal permeability (Peff, cm/s) by 4.45 folds with SDs. Thus, EXM-PEG 6000 SDs showed improved solubility and permeability.

Sphenopalatine ganglion block for relieving postdural puncture headache: technique and mechanism of action of block with a narrative review of efficacy

( Abhijit S. Nair ),( Basanth Kumar Rayani ) 대한통증학회 2017 The Korean Journal of Pain Vol.30 No.2

The sphenopalatine ganglion (SPG) is a parasympathetic ganglion, located in the pterygopalatine fossa. The SPG block has been used for a long time for treating headaches of varying etiologies. For anesthesiologists, treating postdural puncture headaches (PDPH) has always been challenging. The epidural block patch (EBP) was the only option until researchers explored the role of the SPG block as a relatively simple and effective way to treat PDPH. Also, since the existing evidence proving the efficacy of the SPG block in PDPH is scarce, the block cannot be offered to all patients. EBP can be still considered if an SPG block is not able to alleviate pain due to PDPH. (Korean J Pain 2017; 30: 93-7)

A Gelucire 44/14 and labrasol based solid self emulsifying drug delivery system: formulation and evaluation

Venkata Raman Kallakunta,Basanth Babu Eedara,Raju Jukanti,Ram Kishan Ajmeera,Suresh Bandari 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.3

A solid self emulsifying formulation (S-SEF)has been developed with an intention to improve the dissolution characteristics of poorly water soluble lercanidipine hydrochloride (LH). Suitable components for the formulation of liquid self emulsifying drug delivery systems (SEDDS) were selected after screening various vehicles via solubility studies. Formulations were designed with Gelucire 44/14 as oil, labrasol as surfactant and transcutol-P as co surfactant. The prepared formulations were evaluated for self emulsifying efficiency and ternary phase diagram was used to designate optimum systems in the emulsifying domain. These systems were further investigated for robustness towards different pH conditions,globule size, thermodynamic stability, surface morphology,cloud point and in vitro drug release. The optimized LH loaded formulation possessed a mean globule size of 142.5 ± 5.37 nm and cloud point of 72 ±2.66 C. The liquid SEDDS was transformed into free flowing S-SEF by adsorbing on to an inert carrier, Neusilin US2. The results revealed no difference in globule size and emulsification characteristics between liquid SEDDS and S-SEF. The solid state characterization studies indicated loss of crystallinity for the drug. Significant improvement in dissolution characteristics of LH for prepared S-SEF was observed compared with pure drug.

Biocompatible biodegradable polymeric nanocarriers in dry powder inhalers (DPIs) for pulmonary inhalation delivery

Encinas-Basurto David,Eedara Basanth Babu,Mansour Heidi M. 한국약제학회 2024 Journal of Pharmaceutical Investigation Vol.54 No.2

Background Pulmonary drug delivery is an efficient way to deliver drugs directly to the site of action i.e., lungs or to the blood circulation with minimum systemic effects. Recent emergence of coronavirus disease-2019 (COVID-19) and expeditious development of nanoparticle-based vaccines have recently reignited considerable interest in designing inhalable nanoparticle-based drug delivery systems as next-generation respiratory therapeutics. Area covered In this review, dry powder inhaler (DPI) formulations based on polymeric nanoparticles have been reviewed. It comprehensively describes various biodegradable and biocompatible synthetic (e.g. polylactic-glycolic acid, polyethylene glycol, polyethylenimine, and polycaprolactone) and natural (e.g. alginate, chitosan, dextran, hyaluronic acid, and gelatin) polymers used in formulating nanoparticle-based dry powder inhalers. This review covers the most recent drugs encapsulated in synthetic-based and natural-based biocompatible nanocarriers used in DPIs, providing latest approaches for treating various respiratory and pulmonary disorders. Expert Opinion DPIs comprised of biocompatible biodegradable polymeric nanocarriers exhibited favorable particle properties and aerodynamic properties. In addition, these polymeric nanocarriers are chemically versatile in being either synthetic or natural. This chemical versatility enables versatility in the various types of drugs that can be incorporated into DPIs provided that the needed particle properties and aerodynamic properties are maintained.

Preparation and characterization of docetaxel self-nanoemulsifying powders (SNEPs): A strategy for improved oral delivery

Suresh Bandari,Sharath Sunkavalli,Basanth Babu Eedara,Karthik Yadav Janga,Ashok Velpula,Raju Jukanti 한국화학공학회 2016 Korean Journal of Chemical Engineering Vol.33 No.3

Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) of docetaxel were prepared using varying ratios of Capmul PG 8 NF (oil), Cremophor EL (surfactant) and Transcutol-P (co-surfactant). The optimized L-SNEDDS (L11) was transformed into self-nanoemulsifying powder (SNEP) by physical adsorption on to Neusilin US2 and evaluated for dissolution behavior, in vitro cytotoxicity and in vivo oral bioavailability. Optimized L-SNEDDS (L11) composed of 50% of oil, 41.7% of surfactant and 8.3% co-surfactant produced stable emulsion with smaller globules (43±3 nm). In vitro dissolution studies showed the rapid drug release within 5min (95.42±1%) from SNEPN. In vitro cytotoxicity assessed by the MTT assay using MCF-7 human breast cancer cell lines revealed that L-SNEDDS significantly reduced the IC50 value and was 2.3 times lower than the pure docetaxel. Further, the oral bioavailability studies in male Wistar rats showed higher Cmax values following treatment with SNEPN (0.98±0.13 μg/mL) and L-SNEDDS (1.09± 0.06 μg/mL) compared to pure docetaxel (0.37±0.04 μg/mL).

Proliposomes of lisinopril dihydrate for transdermal delivery: Formulation aspects and evaluation

Suresh Bandari,Swetha Gangishetty,Basanth Babu Eedara,Raju Jukanti,Prabhakar Reddy Veerareddy 한국화학공학회 2013 Korean Journal of Chemical Engineering Vol.30 No.8

We formulated and evaluated proliposomal gel of relatively low bioavailable drug lisinopril dihydrate (LDH)for transdermal delivery. Several proliposomal gel formulations of lisinopril dihydrate were prepared by modified coacervation phase separation method and examined for formation of liposomes by optical microscope and characterized by transmission electron microscopy. The formulations were evaluated for size, zeta potential, entrapment efficiency,rheological behavior, ex vivo drug permeation, skin irritation and stability. Differential scanning calorimetry (DSC)and Fourier transform infrared (FTIR) studies were performed to understand the phase transition behavior and mechanism for skin permeation, respectively. The microscopic examination revealed the formation of liposomes from proliposomal gel, and the size of the vesicles was found to be in the range of 385 nm to 635 nm. Entrapment efficiency was high for the formulation containing greater amounts of phosphatidylcholine. The DSC studies indicated the amorphous form of LDH in proliposomal gel formulation. Ex vivo permeation studies revealed sustained permeation of drug from proliposomal gels studied. The stability studies reveal that the proliposomal formulations are more stable when stored at refrigeration temperature (4 oC). In conclusion, proliposomal gels offer potential and prove to be efficient carriers for improved and sustained transdermal delivery of lisinopril dihydrate.

Physicochemical characterization and dissolution enhancement of loratadine by solid dispersion technique

Suresh Bandari,Subash Jadav,Basanth Babu Eedara,Raju Jukanti,Prabhakar Reddy Veerareddy 한국화학공학회 2013 Korean Journal of Chemical Engineering Vol.30 No.1

The purpose of this investigation was to enhance the dissolution rate of loratadine using polyethylene glycol 6000 (PEG) solid dispersions (SDs). The solubility behavior of loratadine in the presence of polyethylene glycol 4000and polyethylene glycol 6000 in water showed linear increase with increasing concentrations of PEG, indicating AL type solubility diagrams. SDs of loratadine with PEG 6000 were prepared at 1 : 1, 1 : 3, 1 : 5, 1 : 7 and 1 : 9 ratios by the solvent evaporation method. Solid dispersions were characterized for drug content, dissolution behavior and for physicochemical characteristics. The dissolution rate of loratadine was enhanced rapidly with increasing concentrations of PEG 6000 in SDs. Fourier transform infrared (FTIR) studies showed the stability of loratadine and the absence of a well-defined loratadine - PEG 6000 interaction. Differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRD) studies revealed the amorphous state of loratadine in SDs of loratadine with PEG 6000 which was further confirmed from scanning electron microscopy (SEM) studies. The flow properties of the blend, physical characteristics and disintegration time of the tablets formulated indicated that PEG 6000 SD can be used to formulate fast release loratadine tablets.

Development and preliminary characterization of levofloxacin pharmaceutical cocrystals for dissolution rate enhancement

Suresh Bandari,Venkateshwara Rao Dronam,Basanth Babu Eedara 한국약제학회 2017 Journal of Pharmaceutical Investigation Vol.47 No.6

The current investigation aimed to enhance the dissolution rate and mask the bitter taste of levofloxacin by developing pharmaceutical cocrystals using stearic acid and saccharin sodium as coformers. The developed cocrystals were characterized by Fourier transform infrared spectroscopy, which showed the formation of a regular carboxylic acid homosynthon in 1:1 ratio of levofloxacinstearic acid and carboxylic acid- imide heterosynthon in 2:1 ratio of levofloxacin-saccharin sodium. The existence of the drug in a new crystalline form in the developed cocrystals was confirmed by solid state characterization. The dissolution studies of the developed cocrystals in simulated gastric fluid (pH 1.2) showed significant improvement of the drug dissolution rate (%min−1) from L-ST1 (7.8 ± 0.1) and L-SA2 (7.2 ± 0.4) cocrystals compared to supplied levofloxacin (4.4 ± 0.3). The taste masking ability of L-ST1 and L-SA2 was determined by conducting dissolution studies at salivary pH 6.6 and the results showed a very low drug release of 6.6 ± 0.6% from L-ST1 compared to supplied levofloxacin (64.5 ± 1.5%) and L-SA2 (55.1 ± 1.5%) in 5 min. This study demonstrates that pharmaceutical cocrystals of levofloxacin with stearic acid at 1:1 ratio enhanced the dissolution rate and masked the bitter taste of levofloxacin whereas saccharin sodium has showed only improved dissolution.

Efficacy of bilateral greater occipital nerve block in postdural puncture headache: a narrative review

( Abhijit S. Nair ),( Praveen Kumar Kodisharapu ),( Poornachand Anne ),( Mohammad Salman Saifuddin ),( Christopher Asiel ),( Basanth Kumar Rayani ) 대한통증학회 2018 The Korean Journal of Pain Vol.31 No.2

The Epidural blood patch is considered the gold standard for managing postdural puncture headache when supportive measures fail. However, it is a procedure which can lead to another inadvertent dural puncture. Other potential adverse events that could occur during a blood patch are meningitis, neurological deficits, and unconsciousness. The bilateral greater occipital nerve block has been used for treating chronic headaches in patients with PDPH with a single injection. This minimally invasive, simple procedure can be considered for patients early, along with other supportive treatment, and an epidural blood patch can be avoided. (Korean J Pain 2018; 31: 80-6)